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Epigenetic Reader Domain

Isoform-selective Products

BET p300/CBP BRPF bromodomain

Signaling Pathway

Epigenetic Reader Domain Products

All (91)
Epigenetic Reader Domain Inhibitors (84)
Epigenetic Reader Domain Activators (2)
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Epigenetic Reader Domain Modulator (1)
New Epigenetic Reader Domain Products

Catalog No.	Product Name	Information	Product Use Citations
S7110	(+)-JQ1	(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.	Nat Immunol, 2024, 25(9):1580-1592 Gastroenterology, 2024, S0016-5085(24)00062-3 ACS Nano, 2024, 18(39):26614-26630
S1109	BI 2536	BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.	Leukemia, 2024, 38(5):969-980 Clin Transl Med, 2024, 14(5):e1703 Clin Transl Med, 2024, 14(5):e1703
S2662	ICG-001	ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. ICG-001 induces apoptosis.	Nat Commun, 2024, 15(1):2551 Int J Biol Sci, 2024, 20(3):848-863 Cell Death Dis, 2024, 15(5):332
S7152	C646	C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a K_i of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.	Nat Commun, 2024, 15(1):5209 Cell Commun Signal, 2024, 22(1):117 Antioxidants (Basel), 2024, 13(4)424
S7360	Birabresib (OTX015)	Birabresib (OTX015, MK 8628) is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Birabresib inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.	Gastroenterology, 2024, S0016-5085(24)00062-3 Cell Death Dis, 2024, 15(8):603 Sci Rep, 2024, 14(1):9284
S2780	I-BET151 (GSK1210151A)	I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively.	Br J Cancer, 2024, 10.1038/s41416-024-02740-5 Cell Rep Methods, 2024, S2667-2375(24)00094-8 bioRxiv, 2024, 2024.08.30.610517
S1848	Curcumin	Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase（IC50~25 μM）and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.	Cancer Cell Int, 2024, 24(1):303 Front Pharmacol, 2024, 15:1418902 PLoS Negl Trop Dis, 2024, 18(8):e0012428
S7189	Molibresib (I-BET-762)	Molibresib (I-BET-762, GSK525762, GSK525762A) is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins.	Cells, 2024, 13(13)1108 EBioMedicine, 2023, 95:104752 EBioMedicine, 2023, 95:104752
S7525	XMD8-92	XMD8-92 is a potent and selective dual inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET) with K_d of 80 nM and 170 nM for ERK5 and BRD4(1), respectively.	Stem Cell Reports, 2024, S2213-6711(24)00216-9 Mol Biol Rep, 2024, 51(1):313 Nat Commun, 2023, 10.1038/s41467-023-43369-x
S7256	SGC-CBP30	SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively.	Cell Syst, 2023, 14(6):482-500.e8 Cell Rep, 2023, 42(8):112963 Cell Rep, 2023, 42(6):112547
S8968	PRI-724	PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.	Adv Sci (Weinh), 2024, 11(35):e2308417 Cell Rep, 2024, 43(7):114414 Nat Commun, 2023, 14(1):4671
S7582	Anacardic Acid	Anacardic Acid (6-pentadecylsalicylic Acid) is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases, which also has antibacterial activity, antimicrobial activity, prostaglandin synthase inhibition, and tyrosinase and lipoxygenase inhibition.	Int J Mol Sci, 2024, 25(17)9600 POLYU ELECTRONIC THESES, 2023, viii, 164 Hepatology, 2021, 10.1002/hep.32245
S8496	EED226	EED226 is a potent, selective, and orally bioavailable a novel allosteric Polycomb repressive complex 2 (PRC2) inhibitor with an IC50 of 23.4 nM when the H3K27me0 peptide was used as substrate and an IC50 of 53.5 nM when the mononucleosome was used as the substrate. It directly binds to the H3K27me3 binding pocket of EED.	Elife, 2023, 12e85365 Elife, 2023, 12e85365 Open Biol, 2023, 13(1):220211
S7295	Apabetalone (RVX-208)	Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.	Sci Adv, 2023, 9(15):eade3422 Sci Adv, 2023, 9(15):eade3422 Biomed Pharmacother, 2022, 152:113230
S8740	A-485	A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets.	Cell Rep, 2024, 43(8):114529 Ecotoxicol Environ Saf, 2024, 270:115877 Cancers (Basel), 2024, 16(9)1622
S8409	KG-501	KG-501 is a cAMP response element-binding protein (CREB) inhibitor that disrupts CREB-dependent transcription (Ki = 10 μM) and CREB:CBP interaction (Ki = 50 μM). It also disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ≈90 μM, using concentrations of CREB that were within the linear range of the binding assay.	Front Oncol, 2023, 13:1082441 Front Oncol, 2023, 13:1082441 Cell Death Differ, 2022, 10.1038/s41418-022-01053-5
S7304	CPI-203	CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.	Cell Chem Biol, 2023, 30(8):987-998.e24 Microbiol Spectr, 2022, 10(4):e0241921 Mol Cancer Ther, 2021, molcanther.0809.2020
S8846	compound 3i (666-15)	Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells.	J Virol, 2024, 98(4):e0156523 Theranostics, 2023, 13(4):1355-1369 J Exp Clin Cancer Res, 2023, 42(1):25
S7315	PFI-3	PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.	Cell Rep, 2023, 42(2):112097 J Transl Med, 2023, 21(1):639 J Transl Med, 2023, 21(1):639
S8344	AZD5153 6-hydroxy-2-naphthoic acid	AZD5153 6-hydroxy-2-naphthoic acid (HNT salt) is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4. AZD5153 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. NSD3, via H3K36me2, acts as an epigenetic deregulator to facilitate the expression of oncogenesis-promoting genes.	J Immunother Cancer, 2023, 11(4)e006070 J Immunother Cancer, 2023, 11(4)e006070 Res Sq, 2023, 10.21203/rs.3.rs-3314138/v1
S1216	PFI-1 (PF-6405761)	PFI-1 (PF-6405761) is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay.	Proc Natl Acad Sci U S A, 2023, 120(4):e2218118120 MedComm (2020), 2022, 3(3):e152 Cell Death Dis, 2022, 13(10):912
S8400	Mivebresib (ABBV-075)	Mivebresib (ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumor cell.	Cell Commun Signal, 2024, 22(1):415 Cancers (Basel), 2024, 16(6)1125 Transl Androl Urol, 2024, 13(6):1014-1023
S8762	dBET6	dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis.	J Nanobiotechnology, 2024, 22(1):692 J Pathol, 2024, 262(1):37-49 Genes Cancer, 2023, 10.18632/genesandcancer.233
S8723	ABBV-744	ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2, BRD3 and BRD4. It is developed for treating AML and cancers.	Cancers (Basel), 2023, 16(1)107 Invest Ophthalmol Vis Sci, 2023, 64(7):9 Nat Cell Biol, 2022, 24(1):24-34
S7088	UNC1215	UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and K_d of 120 nM, 50-fold selective versus other members of the human MBT family.	Cell Rep, 2022, 39(12):110994 Cancers (Basel), 2022, 14(19)4883 Cell Death Differ, 2021, 28(8):2536-2551
S7835	I-BRD9	I-BRD9 (GSK602) is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4.	Int J Mol Sci, 2024, 25(2)905 PLoS Pathog, 2022, 18(12):e1011039 Pigment Cell Melanoma Res, 2022, 10.1111/pcmr.13068
S7233	Bromosporine	Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.	J Med Chem, 2022, 65(5):4182-4200 Front Oncol, 2022, 12:1011173 Cancer Res, 2018, 78(20):5731-5740
S8739	PLX51107	PLX51107 is as a novel BET inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2) within each BET protein (Kd = 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1 and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively. Among non-BET proteins, PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range).	Int J Mol Sci, 2023, 24(8)7623 Int J Mol Sci, 2023, 24(8)7623 Microbiol Spectr, 2022, 10(4):e0241921
S7620	GSK1324726A (I-BET726)	GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively.	Am J Cancer Res, 2023, 13(11):5382-5393 Cancers (Basel), 2022, 14(11)2755 Front Oncol, 2021, 11:773186
S7853	Pelabresib (CPI-0610)	Pelabresib (CPI-0610) is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with an IC50 of 39 nM for BRD4-BD1 in TR-FRET assay and currently undergoing human clinical trials for hematological malignancies. CPI-0610 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.	Cell Death Dis, 2024, 15(8):603 Inflammation, 2022, 45(3):1388-1401 Inflammation, 2022, 45(3):1388-1401
S8297	ARV-825	ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.	Gastroenterology, 2024, S0016-5085(24)00062-3 bioRxiv, 2024, 2024.05.10.593637 PLoS Pathog, 2023, 19(9):e1011657
S8180	PF-CBP1 HCl	PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.	Nat Commun, 2022, 13-1:6117 Nat Aging, 2021, 1(2):165-178 Cancer Res, 2018, 78(2):436-450
S8753	INCB054329	INCB054329 is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively.	Cell Death Dis, 2024, 15(8):603 Microbiol Spectr, 2022, 10(4):e0241921 Cell, 2021, S0092-8674(21)00354-8
S7305	MS436	MS436 is a selective BET bromodomain inhibitor with K_i of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively.	Microbiol Spectr, 2022, 10(4):e0241921 Cancer Res, 2018, 78(20):5731-5740 Cell Physiol Biochem, 2018, 50(2):640-653
S7373	UNC669	UNC669 is a potent and selective MBT (malignant brain tumor) inhibitor with IC50 of 6 μM for L3MBTL1, 5- and 11-fold selective over L3MBTL3 and L3MBTL4.	J Med Chem, 2020, 31 Cancer Res, 2018, 78(20):5731-5740 Lab Invest, 2018, 98(12):1627-1641
S7231	GSK2801	GSK2801 is a selective bromodomains BAZ2A/B inhibitor with K_D of 257 nM and 136 nM, respectively.	Int J Mol Sci, 2023, 24(6)5993 Epigenetics, 2019, 10.1080/15592294.2019.1656156 Cancer Res, 2018, 78(20):5731-5740
S8589	SF2523	SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.	Mol Ther Nucleic Acids, 2023, 31:309-323 Cell Biol Int, 2022, 10.1002/cbin.11833 Oncotarget, 2017, 8(58):98471-98481
S8889	MZ-1	MZ-1 is a PROTAC degrader of bromodomain-containing protein 4 (BRD4). MZ-1 binds to the Brd bromodomain with Kd of 62 nM, 60 nM, 21 nM, 13 nM, 39 nM and 15 nM for Brd2^BD1, Brd2^BD2, Brd3^BD1, Brd3^BD2, Brd4^BD1 and Brd4^BD2.	Antiviral Res, 2023, 211:105552 Int Immunopharmacol, 2023, 117:109929 Cancers (Basel), 2021, 13(16)4118
S9648	NEO2734	NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM.	Cell Rep Med, 2024, 5(3):101471 Nat Cancer, 2023, 4(10):1508-1525 PLoS Pathog, 2023, 19(8):e1011598
S8296	dBET1	dBET1 is a CRBN-based BET degrader with an IC50 of 20 nM, showing highly selectivity. Out of 7,429 proteins, only the expression of the oncoproteins MYC and PIM1, as well as BRD2, BRD3 and BRD4 are significantly downregulated by dBET1 treatment.	Exp Ther Med, 2023, 10.3892/etm.2023.12241 Exp Ther Med, 2023, 26(5):542 Methods Mol Biol, 2021, 2365:3-20
S7681	OF-1	OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with K_d of 100 nM and 500 nM, respectively.	Cell Rep, 2021, 35(11):109233 J Mol Cell Biol, 2020, 11;12(5):359-371 Cancer Res, 2018, 78(20):5731-5740
S8190	CPI-637	CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM and 0.051μM for CBP and EP300 respectively in TR-FRET assay. It is highly selective against other bromodomains, displaying substantial biochemical activity only against BRD9.	Mol Cell Proteomics, 2023, 22(3):100504 Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0237-5
S8265	GSK6853	GSK6853 is a selective benzimidazolone BRPF1 inhibitor with pIC50 of 8.1(TR-FRET) showing greater than 1600-fold selectivity over all other bromodomains tested.	Front Oncol, 2021, 11:766656 J Mol Cell Biol, 2020, 11;12(5):359-371
S6758	I-CBP112	I-CBP112 is a potent and selective CBP/p300 inhibitor with dissociation constant (KD) of 151 ± 6 nM and 167 ± 8 nM for CBP and p300, respectively.	Hepatology, 2021, 10.1002/hep.32245 Hepatology, 2021, 10.1002/hep.32245
S8179	BI-7273	BI-7273 is a potent, selective, and cell-permeable BRD9 BD inhibitor with IC50s of 19 nM and 117 nM for BRD9 and BRD7 respectively in alpha assay.	Cancer Res, 2018, 78(20):5731-5740
S0022	YF-2	YF-2 is a highly selective, blood-brain-barrier permeable activator of histone acetyltransferase (HAT). In In vitro assays, YF-2 has activity versus CBP, PCAF, and GCN5 with EC50 of 2.75 μΜ, 29.04 μΜ and 49.3 μΜ, respectively. YF-2 also increases p300 activity.	J Exp Clin Cancer Res, 2022, 41(1):77
S7906	PFI-4	PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.	J Mol Cell Biol, 2020, 11;12(5):359-371
S8714	INCB057643	INCB057643 is a BET inhibitor that binds to the acetylated lysine recognition motifs found in the BRD of BET proteins, thereby preventing the interaction between the BET proteins and acetylated lysines on histones.	Sci Rep, 2023, 13(1):18554
S5916	GSK 5959	GSK5959 is a potent and selective BRPF1 bromodomain inhibitor with an IC50 of 80 nM and exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.	Life Sci Alliance, 2023, 6(10)e202302009
S0137	dBET57	dBET57 is a novel, potent and selective degrader of BRD4_BD1 based on the PROTAC technology with DC_50/5h of 500 nM. dBET57 is inactive on BRD4_BD2.	J Immunol Res, 2022, 2022:7945884
S8113	BI-9564	BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains with the IC50 of 75 nM and 3.4 µM, respectively.	Mol Cancer Res, 2019, 17(7):1503-1518
S1161	Histone Acetyltransferase Inhibitor II	Histone Acetyltransferase Inhibitor II (HAT Inhibitor II, compound 2c) is a potent, selective and cell-permeable p300 histone acetyltransferase (HAT) inhibitor with IC50 of 5 μM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.	Genetics, 2017, 205(3):1125-1137
S3984	Nordihydroguaiaretic acid (NDGA)	Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis.
S8961	Alobresib (GS-5829)	Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling.
S5262	UNC-926	UNC-926 is a L3MBTL1 domain inhibitor with Kd value of 3.9 μM for binding with the MBT domain of the L3MBTL1 protein.
S8785	A1874	A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency.
S8665	GNE-781	GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity.	Viruses, 2024, 16(5)775 PLoS Pathog, 2023, 19(8):e1011598
S9691	BMS-986158	BMS-986158 is a potent inhibitor of BET with IC50s of 6.6 nM and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.
E1932^New	DW71177	DW71177 is a potent BD1-Selective inhibitor of BET. DW71177 selectively interacts with BD1 and exhibits strong antileukemic activity. DW71177 can also be used in the study of acute myeloid leukemia.
E1517	ZEN-3694	ZEN-3694 is an orally bioavailable bromodomain extraterminal inhibitor (BETi) that leads to down-regulation of expression of AR-signaling in metastatic castrationresistant prostate cancer (mCRPC) models.
S8763	ZL0420	ZL0420 is a potent and selective BRD4 inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 respectively and good selectivity over that of the related BRD2 homolog.
E0494	NI-42	NI-42 is a biased, potent inhibitor of the of the bromodomain and PHD finger-containing (BRPF) with IC50s of 7.9, 48, 260 nM for BRPF1/2/3.
S8625^New	GNE-049	GNE-049 is a highly potent and selective inhibitor of CBP. It exhibits an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also effectively inhibits BRET and BRD4 with IC50 values of 12 nM and 4200 nM, respectively.
E1095	ODM-207	ODM-207 is a potent and selective BET inhibitor that is structurally unrelated to the benzodiazepine. ODM-207 also shows potent antiproliferative effects in patient-derived cancer cells and in xenograft models.
S1027	FL-411	FL-411 (BRD4-IN-1) is a potent and selective inhibitor of Bromodomain-containing protein 4 (BRD4) with IC50 of 0.43 μM for BRD4(1). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction.
E1683^New	DN02	DN02 is a selective probe of BRD8 bromodomain family. It exhibits potency against BRD8(1) with a Kd of 32 nM, and interestingly, demonstrated this activity to be selective over BRD8's second bromodomain (BRD8(2) with a Kd of >1000 nM)
S0344	Y06036	Y06036 (Compound 6i) is a potent and selective inhibitor of BET with antitumor activity. Y06036 binds to the BRD4(1) bromodomain with Kd of 82 nM.
E1859^New	FHD-609	FHD-609 acts as a selective inhibitor and degrader of BRD9 protein (bromodomain-containing protein 9). FHD-609 targets ncBAF and can be used in research of various cancers involving mutations in a BAF complex subunit.
S8948	SRX3207	SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity.
S7615^New	MS417	MS417 (GTPL7512) is a selective inhibitor of BET-specific BRD4. MS417 binds to BRD4-BD1 and BRD4-BD2 with IC50 values of 30 nM and 46 nM and Kd values of 36.1 nM, and 25.4 nM, respectively. MS417 effectively blocks BRD4 binding to the acetylated NF-κB and attenuates NF-κB transcriptional activation of proinflammatory genes in kidney cells treated with TNFα.
E1348	E-7386	E-7386 is a selective inhibitor which inhibits interaction between CBP/beta-catenin with IC50 value of 0.0484 μM in HEK293 cells.	Adv Sci (Weinh), 2024, 11(35):e2308417 Cell Rep, 2024, 43(8):114532
S3573	Trotabresib (CC-90010)	Trotabresib (CC-90010) is a reversible, orally active and central nervous system-penetrant inhibitor of bromodomain and extra-terminal (BET) proteins. CC-90010 is applied in the study for advanced solid tumors.	Cell Rep Med, 2024, 5(3):101471
E1144	dBRD9	dBRD9 is a bifunctional molecule that links a small molecule that specifically binds to the bromodomain of BRD9 and another ligand that recruits the cereblon E3 ubiquitin ligase, potently and selectively degrades BRD9 with IC50 of 104 nM in MOLM-13 cells.
E0807	NHWD-870	NHWD-870 inhibits CSF1 expression through suppressing BRD4 and its target HIF1α.
S9667	Inobrodib (CCS-1477)	Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4）is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.	bioRxiv, 2024, 2024.03.29.587346 PLoS Pathog, 2023, 19(8):e1011598
E1664^New	GNE-987	GNE-987 is a BRD4-degradating PROTAC consisting of BRD4B1 and BRD4B2 (BRD4 bromodomains 1 and 2) and the VHL E3-ubiquitin ligase. It exhibits BRD4 degradation activity with DC50 of 0.03 nM for the EOL-1 AML cell line. GNE-987 inhibits cell proliferation and induces apoptosis by promoting the rapid and sustained degradation of BRD4 and inhibiting its downstream targets. It also demonstrates potent antitumor activity in AML cell lines.
S9659	UNC6852	UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. UNC6852 is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL.
S2941	(+)-JQ1 PA	(+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1.
S2943	BRD9539	BRD9539 is a histone methyltransferase G9a inhibitor, which also inhibits PRC2 activity.
E4609^New	Amredobresib	Amredobresib (BI894999) is an oral inhibitor of BET, which acts as an acetyl-lysine mimic. It prevents the bromodomains BRD4-BD1 and BRD4-BD2 from binding to acetylated histones, with an IC50 of 5 nM for BRD4-BD1 and 41 nM for BRD4-BD2.
S8574	BRD4 Inhibitor-10	BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor with an IC50 of 8 nM.
S8545	TEN-010 ((S)-JQ-35)	TEN-010 (RG6146, Ro-6870810,(S)-JQ-35) is an inhibitor of the Bromodomain and Extra-Terminal(BET) family bromodomain-containing proteins with potential antineoplastic activity.
E1177	CFT8634	CFT8634 is a potent BRD9 degrader with DC50 of 3 nM. It forms a ternary complex with BRD9 and an E3 ligase, resulting in BRD9 ubiquitination. CFT8634 is used in the treatment of SMARCB1-perturbed cancers.
S9683	GSK778 (iBET-BD1)	GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75 nM for BRD2 BD1, 41 nM for BRD3 BD1, 41 nM for BRD4 BD1, and 143 nM for BRDT BD1.
S6397	Thalidomide-NH-C4-NH-Boc	Thalidomide-NH-C4-NH-Boc is a novel, potent, and selective class of Bromodomain-containing protein 4 (BRD4) and Bromodomain-containing protein 2 (BRD2) degrader for the development of therapeutics to treat cancers.
S9684	GSK046 (iBET-BD2)	GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET (bromodomain and extraterminal domain) with IC50 of 264 nM, 98 nM, 49 nM and 214 nM for BRD2_BD2, BRD3_BD2, BRD4_BD2 and BRDT_BD2, respectively. GSK046 exhibits immunomodulatory activity.
S9685	GSK620	GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.
E0449	SGC-SMARCA-BRDVIII	SGC-SMARCA-BRDVIII is a potent and selective SMARCA2/4 BRD inhibitor.
S2966^New	TTK21	TTK21 is an activator of the histone acetyltransferases CBP/p300. It activates CBP/p300 histone acetyltransferase activity in a concentration-dependent manner with a maximal effect at a concentration of 275 µM. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different brain parts when conjugated to glucose-based carbon nanosphere (CSP).
E0781	BAZ1A-IN-1	BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein), exerting a Kd value of 0.52 μM against BAZ1A bromodomain, shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A.
E1711^New	FHT-1015	FHT-1015 is a potent, small-molecule, allosteric inhibitor of SMARCA4/SMARCA2 ATPase with IC50 values ≤10 nM. FHT-1205 decreases PD1+TIM3+ cells and cytokine expression in vivo.
S7110	(+)-JQ1	(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.	Nat Immunol, 2024, 25(9):1580-1592 Gastroenterology, 2024, S0016-5085(24)00062-3 ACS Nano, 2024, 18(39):26614-26630
S1109	BI 2536	BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.	Leukemia, 2024, 38(5):969-980 Clin Transl Med, 2024, 14(5):e1703 Clin Transl Med, 2024, 14(5):e1703
S2662	ICG-001	ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. ICG-001 induces apoptosis.	Nat Commun, 2024, 15(1):2551 Int J Biol Sci, 2024, 20(3):848-863 Cell Death Dis, 2024, 15(5):332
S7152	C646	C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a K_i of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.	Nat Commun, 2024, 15(1):5209 Cell Commun Signal, 2024, 22(1):117 Antioxidants (Basel), 2024, 13(4)424
S7360	Birabresib (OTX015)	Birabresib (OTX015, MK 8628) is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Birabresib inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.	Gastroenterology, 2024, S0016-5085(24)00062-3 Cell Death Dis, 2024, 15(8):603 Sci Rep, 2024, 14(1):9284
S2780	I-BET151 (GSK1210151A)	I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively.	Br J Cancer, 2024, 10.1038/s41416-024-02740-5 Cell Rep Methods, 2024, S2667-2375(24)00094-8 bioRxiv, 2024, 2024.08.30.610517
S1848	Curcumin	Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase（IC50~25 μM）and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.	Cancer Cell Int, 2024, 24(1):303 Front Pharmacol, 2024, 15:1418902 PLoS Negl Trop Dis, 2024, 18(8):e0012428
S7189	Molibresib (I-BET-762)	Molibresib (I-BET-762, GSK525762, GSK525762A) is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins.	Cells, 2024, 13(13)1108 EBioMedicine, 2023, 95:104752 EBioMedicine, 2023, 95:104752
S7525	XMD8-92	XMD8-92 is a potent and selective dual inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET) with K_d of 80 nM and 170 nM for ERK5 and BRD4(1), respectively.	Stem Cell Reports, 2024, S2213-6711(24)00216-9 Mol Biol Rep, 2024, 51(1):313 Nat Commun, 2023, 10.1038/s41467-023-43369-x
S7256	SGC-CBP30	SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively.	Cell Syst, 2023, 14(6):482-500.e8 Cell Rep, 2023, 42(8):112963 Cell Rep, 2023, 42(6):112547
S8968	PRI-724	PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.	Adv Sci (Weinh), 2024, 11(35):e2308417 Cell Rep, 2024, 43(7):114414 Nat Commun, 2023, 14(1):4671
S7582	Anacardic Acid	Anacardic Acid (6-pentadecylsalicylic Acid) is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases, which also has antibacterial activity, antimicrobial activity, prostaglandin synthase inhibition, and tyrosinase and lipoxygenase inhibition.	Int J Mol Sci, 2024, 25(17)9600 POLYU ELECTRONIC THESES, 2023, viii, 164 Hepatology, 2021, 10.1002/hep.32245
S8496	EED226	EED226 is a potent, selective, and orally bioavailable a novel allosteric Polycomb repressive complex 2 (PRC2) inhibitor with an IC50 of 23.4 nM when the H3K27me0 peptide was used as substrate and an IC50 of 53.5 nM when the mononucleosome was used as the substrate. It directly binds to the H3K27me3 binding pocket of EED.	Elife, 2023, 12e85365 Elife, 2023, 12e85365 Open Biol, 2023, 13(1):220211
S7295	Apabetalone (RVX-208)	Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.	Sci Adv, 2023, 9(15):eade3422 Sci Adv, 2023, 9(15):eade3422 Biomed Pharmacother, 2022, 152:113230
S8740	A-485	A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets.	Cell Rep, 2024, 43(8):114529 Ecotoxicol Environ Saf, 2024, 270:115877 Cancers (Basel), 2024, 16(9)1622
S8409	KG-501	KG-501 is a cAMP response element-binding protein (CREB) inhibitor that disrupts CREB-dependent transcription (Ki = 10 μM) and CREB:CBP interaction (Ki = 50 μM). It also disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ≈90 μM, using concentrations of CREB that were within the linear range of the binding assay.	Front Oncol, 2023, 13:1082441 Front Oncol, 2023, 13:1082441 Cell Death Differ, 2022, 10.1038/s41418-022-01053-5
S7304	CPI-203	CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.	Cell Chem Biol, 2023, 30(8):987-998.e24 Microbiol Spectr, 2022, 10(4):e0241921 Mol Cancer Ther, 2021, molcanther.0809.2020
S8846	compound 3i (666-15)	Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells.	J Virol, 2024, 98(4):e0156523 Theranostics, 2023, 13(4):1355-1369 J Exp Clin Cancer Res, 2023, 42(1):25
S7315	PFI-3	PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.	Cell Rep, 2023, 42(2):112097 J Transl Med, 2023, 21(1):639 J Transl Med, 2023, 21(1):639
S8344	AZD5153 6-hydroxy-2-naphthoic acid	AZD5153 6-hydroxy-2-naphthoic acid (HNT salt) is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4. AZD5153 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. NSD3, via H3K36me2, acts as an epigenetic deregulator to facilitate the expression of oncogenesis-promoting genes.	J Immunother Cancer, 2023, 11(4)e006070 J Immunother Cancer, 2023, 11(4)e006070 Res Sq, 2023, 10.21203/rs.3.rs-3314138/v1
S1216	PFI-1 (PF-6405761)	PFI-1 (PF-6405761) is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay.	Proc Natl Acad Sci U S A, 2023, 120(4):e2218118120 MedComm (2020), 2022, 3(3):e152 Cell Death Dis, 2022, 13(10):912
S8400	Mivebresib (ABBV-075)	Mivebresib (ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumor cell.	Cell Commun Signal, 2024, 22(1):415 Cancers (Basel), 2024, 16(6)1125 Transl Androl Urol, 2024, 13(6):1014-1023
S8762	dBET6	dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis.	J Nanobiotechnology, 2024, 22(1):692 J Pathol, 2024, 262(1):37-49 Genes Cancer, 2023, 10.18632/genesandcancer.233
S8723	ABBV-744	ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2, BRD3 and BRD4. It is developed for treating AML and cancers.	Cancers (Basel), 2023, 16(1)107 Invest Ophthalmol Vis Sci, 2023, 64(7):9 Nat Cell Biol, 2022, 24(1):24-34
S7835	I-BRD9	I-BRD9 (GSK602) is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4.	Int J Mol Sci, 2024, 25(2)905 PLoS Pathog, 2022, 18(12):e1011039 Pigment Cell Melanoma Res, 2022, 10.1111/pcmr.13068
S7233	Bromosporine	Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.	J Med Chem, 2022, 65(5):4182-4200 Front Oncol, 2022, 12:1011173 Cancer Res, 2018, 78(20):5731-5740
S8739	PLX51107	PLX51107 is as a novel BET inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2) within each BET protein (Kd = 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1 and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively. Among non-BET proteins, PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range).	Int J Mol Sci, 2023, 24(8)7623 Int J Mol Sci, 2023, 24(8)7623 Microbiol Spectr, 2022, 10(4):e0241921
S7620	GSK1324726A (I-BET726)	GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively.	Am J Cancer Res, 2023, 13(11):5382-5393 Cancers (Basel), 2022, 14(11)2755 Front Oncol, 2021, 11:773186
S7853	Pelabresib (CPI-0610)	Pelabresib (CPI-0610) is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with an IC50 of 39 nM for BRD4-BD1 in TR-FRET assay and currently undergoing human clinical trials for hematological malignancies. CPI-0610 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.	Cell Death Dis, 2024, 15(8):603 Inflammation, 2022, 45(3):1388-1401 Inflammation, 2022, 45(3):1388-1401
S8297	ARV-825	ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.	Gastroenterology, 2024, S0016-5085(24)00062-3 bioRxiv, 2024, 2024.05.10.593637 PLoS Pathog, 2023, 19(9):e1011657
S8180	PF-CBP1 HCl	PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.	Nat Commun, 2022, 13-1:6117 Nat Aging, 2021, 1(2):165-178 Cancer Res, 2018, 78(2):436-450
S8753	INCB054329	INCB054329 is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively.	Cell Death Dis, 2024, 15(8):603 Microbiol Spectr, 2022, 10(4):e0241921 Cell, 2021, S0092-8674(21)00354-8
S7305	MS436	MS436 is a selective BET bromodomain inhibitor with K_i of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively.	Microbiol Spectr, 2022, 10(4):e0241921 Cancer Res, 2018, 78(20):5731-5740 Cell Physiol Biochem, 2018, 50(2):640-653
S7373	UNC669	UNC669 is a potent and selective MBT (malignant brain tumor) inhibitor with IC50 of 6 μM for L3MBTL1, 5- and 11-fold selective over L3MBTL3 and L3MBTL4.	J Med Chem, 2020, 31 Cancer Res, 2018, 78(20):5731-5740 Lab Invest, 2018, 98(12):1627-1641
S7231	GSK2801	GSK2801 is a selective bromodomains BAZ2A/B inhibitor with K_D of 257 nM and 136 nM, respectively.	Int J Mol Sci, 2023, 24(6)5993 Epigenetics, 2019, 10.1080/15592294.2019.1656156 Cancer Res, 2018, 78(20):5731-5740
S8589	SF2523	SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.	Mol Ther Nucleic Acids, 2023, 31:309-323 Cell Biol Int, 2022, 10.1002/cbin.11833 Oncotarget, 2017, 8(58):98471-98481
S9648	NEO2734	NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM.	Cell Rep Med, 2024, 5(3):101471 Nat Cancer, 2023, 4(10):1508-1525 PLoS Pathog, 2023, 19(8):e1011598
S8296	dBET1	dBET1 is a CRBN-based BET degrader with an IC50 of 20 nM, showing highly selectivity. Out of 7,429 proteins, only the expression of the oncoproteins MYC and PIM1, as well as BRD2, BRD3 and BRD4 are significantly downregulated by dBET1 treatment.	Exp Ther Med, 2023, 10.3892/etm.2023.12241 Exp Ther Med, 2023, 26(5):542 Methods Mol Biol, 2021, 2365:3-20
S7681	OF-1	OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with K_d of 100 nM and 500 nM, respectively.	Cell Rep, 2021, 35(11):109233 J Mol Cell Biol, 2020, 11;12(5):359-371 Cancer Res, 2018, 78(20):5731-5740
S8190	CPI-637	CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM and 0.051μM for CBP and EP300 respectively in TR-FRET assay. It is highly selective against other bromodomains, displaying substantial biochemical activity only against BRD9.	Mol Cell Proteomics, 2023, 22(3):100504 Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0237-5
S8265	GSK6853	GSK6853 is a selective benzimidazolone BRPF1 inhibitor with pIC50 of 8.1(TR-FRET) showing greater than 1600-fold selectivity over all other bromodomains tested.	Front Oncol, 2021, 11:766656 J Mol Cell Biol, 2020, 11;12(5):359-371
S6758	I-CBP112	I-CBP112 is a potent and selective CBP/p300 inhibitor with dissociation constant (KD) of 151 ± 6 nM and 167 ± 8 nM for CBP and p300, respectively.	Hepatology, 2021, 10.1002/hep.32245 Hepatology, 2021, 10.1002/hep.32245
S8179	BI-7273	BI-7273 is a potent, selective, and cell-permeable BRD9 BD inhibitor with IC50s of 19 nM and 117 nM for BRD9 and BRD7 respectively in alpha assay.	Cancer Res, 2018, 78(20):5731-5740
S7906	PFI-4	PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.	J Mol Cell Biol, 2020, 11;12(5):359-371
S8714	INCB057643	INCB057643 is a BET inhibitor that binds to the acetylated lysine recognition motifs found in the BRD of BET proteins, thereby preventing the interaction between the BET proteins and acetylated lysines on histones.	Sci Rep, 2023, 13(1):18554
S5916	GSK 5959	GSK5959 is a potent and selective BRPF1 bromodomain inhibitor with an IC50 of 80 nM and exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.	Life Sci Alliance, 2023, 6(10)e202302009
S0137	dBET57	dBET57 is a novel, potent and selective degrader of BRD4_BD1 based on the PROTAC technology with DC_50/5h of 500 nM. dBET57 is inactive on BRD4_BD2.	J Immunol Res, 2022, 2022:7945884
S8113	BI-9564	BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains with the IC50 of 75 nM and 3.4 µM, respectively.	Mol Cancer Res, 2019, 17(7):1503-1518
S1161	Histone Acetyltransferase Inhibitor II	Histone Acetyltransferase Inhibitor II (HAT Inhibitor II, compound 2c) is a potent, selective and cell-permeable p300 histone acetyltransferase (HAT) inhibitor with IC50 of 5 μM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.	Genetics, 2017, 205(3):1125-1137
S3984	Nordihydroguaiaretic acid (NDGA)	Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis.
S8961	Alobresib (GS-5829)	Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling.
S5262	UNC-926	UNC-926 is a L3MBTL1 domain inhibitor with Kd value of 3.9 μM for binding with the MBT domain of the L3MBTL1 protein.
S8785	A1874	A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency.
S8665	GNE-781	GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity.	Viruses, 2024, 16(5)775 PLoS Pathog, 2023, 19(8):e1011598
S9691	BMS-986158	BMS-986158 is a potent inhibitor of BET with IC50s of 6.6 nM and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.
E1932^New	DW71177	DW71177 is a potent BD1-Selective inhibitor of BET. DW71177 selectively interacts with BD1 and exhibits strong antileukemic activity. DW71177 can also be used in the study of acute myeloid leukemia.
E1517	ZEN-3694	ZEN-3694 is an orally bioavailable bromodomain extraterminal inhibitor (BETi) that leads to down-regulation of expression of AR-signaling in metastatic castrationresistant prostate cancer (mCRPC) models.
S8763	ZL0420	ZL0420 is a potent and selective BRD4 inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 respectively and good selectivity over that of the related BRD2 homolog.
E0494	NI-42	NI-42 is a biased, potent inhibitor of the of the bromodomain and PHD finger-containing (BRPF) with IC50s of 7.9, 48, 260 nM for BRPF1/2/3.
S8625^New	GNE-049	GNE-049 is a highly potent and selective inhibitor of CBP. It exhibits an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also effectively inhibits BRET and BRD4 with IC50 values of 12 nM and 4200 nM, respectively.
E1095	ODM-207	ODM-207 is a potent and selective BET inhibitor that is structurally unrelated to the benzodiazepine. ODM-207 also shows potent antiproliferative effects in patient-derived cancer cells and in xenograft models.
S1027	FL-411	FL-411 (BRD4-IN-1) is a potent and selective inhibitor of Bromodomain-containing protein 4 (BRD4) with IC50 of 0.43 μM for BRD4(1). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction.
S0344	Y06036	Y06036 (Compound 6i) is a potent and selective inhibitor of BET with antitumor activity. Y06036 binds to the BRD4(1) bromodomain with Kd of 82 nM.
E1859^New	FHD-609	FHD-609 acts as a selective inhibitor and degrader of BRD9 protein (bromodomain-containing protein 9). FHD-609 targets ncBAF and can be used in research of various cancers involving mutations in a BAF complex subunit.
S8948	SRX3207	SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity.
S7615^New	MS417	MS417 (GTPL7512) is a selective inhibitor of BET-specific BRD4. MS417 binds to BRD4-BD1 and BRD4-BD2 with IC50 values of 30 nM and 46 nM and Kd values of 36.1 nM, and 25.4 nM, respectively. MS417 effectively blocks BRD4 binding to the acetylated NF-κB and attenuates NF-κB transcriptional activation of proinflammatory genes in kidney cells treated with TNFα.
E1348	E-7386	E-7386 is a selective inhibitor which inhibits interaction between CBP/beta-catenin with IC50 value of 0.0484 μM in HEK293 cells.	Adv Sci (Weinh), 2024, 11(35):e2308417 Cell Rep, 2024, 43(8):114532
S3573	Trotabresib (CC-90010)	Trotabresib (CC-90010) is a reversible, orally active and central nervous system-penetrant inhibitor of bromodomain and extra-terminal (BET) proteins. CC-90010 is applied in the study for advanced solid tumors.	Cell Rep Med, 2024, 5(3):101471
E1144	dBRD9	dBRD9 is a bifunctional molecule that links a small molecule that specifically binds to the bromodomain of BRD9 and another ligand that recruits the cereblon E3 ubiquitin ligase, potently and selectively degrades BRD9 with IC50 of 104 nM in MOLM-13 cells.
E0807	NHWD-870	NHWD-870 inhibits CSF1 expression through suppressing BRD4 and its target HIF1α.
S9667	Inobrodib (CCS-1477)	Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4）is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.	bioRxiv, 2024, 2024.03.29.587346 PLoS Pathog, 2023, 19(8):e1011598
S9659	UNC6852	UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. UNC6852 is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL.
S2941	(+)-JQ1 PA	(+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1.
S2943	BRD9539	BRD9539 is a histone methyltransferase G9a inhibitor, which also inhibits PRC2 activity.
E4609^New	Amredobresib	Amredobresib (BI894999) is an oral inhibitor of BET, which acts as an acetyl-lysine mimic. It prevents the bromodomains BRD4-BD1 and BRD4-BD2 from binding to acetylated histones, with an IC50 of 5 nM for BRD4-BD1 and 41 nM for BRD4-BD2.
S8574	BRD4 Inhibitor-10	BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor with an IC50 of 8 nM.
S8545	TEN-010 ((S)-JQ-35)	TEN-010 (RG6146, Ro-6870810,(S)-JQ-35) is an inhibitor of the Bromodomain and Extra-Terminal(BET) family bromodomain-containing proteins with potential antineoplastic activity.
S9683	GSK778 (iBET-BD1)	GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75 nM for BRD2 BD1, 41 nM for BRD3 BD1, 41 nM for BRD4 BD1, and 143 nM for BRDT BD1.
S6397	Thalidomide-NH-C4-NH-Boc	Thalidomide-NH-C4-NH-Boc is a novel, potent, and selective class of Bromodomain-containing protein 4 (BRD4) and Bromodomain-containing protein 2 (BRD2) degrader for the development of therapeutics to treat cancers.
S9684	GSK046 (iBET-BD2)	GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET (bromodomain and extraterminal domain) with IC50 of 264 nM, 98 nM, 49 nM and 214 nM for BRD2_BD2, BRD3_BD2, BRD4_BD2 and BRDT_BD2, respectively. GSK046 exhibits immunomodulatory activity.
S9685	GSK620	GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.
E0449	SGC-SMARCA-BRDVIII	SGC-SMARCA-BRDVIII is a potent and selective SMARCA2/4 BRD inhibitor.
E0781	BAZ1A-IN-1	BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein), exerting a Kd value of 0.52 μM against BAZ1A bromodomain, shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A.
E1711^New	FHT-1015	FHT-1015 is a potent, small-molecule, allosteric inhibitor of SMARCA4/SMARCA2 ATPase with IC50 values ≤10 nM. FHT-1205 decreases PD1+TIM3+ cells and cytokine expression in vivo.
S0022	YF-2	YF-2 is a highly selective, blood-brain-barrier permeable activator of histone acetyltransferase (HAT). In In vitro assays, YF-2 has activity versus CBP, PCAF, and GCN5 with EC50 of 2.75 μΜ, 29.04 μΜ and 49.3 μΜ, respectively. YF-2 also increases p300 activity.	J Exp Clin Cancer Res, 2022, 41(1):77
S2966^New	TTK21	TTK21 is an activator of the histone acetyltransferases CBP/p300. It activates CBP/p300 histone acetyltransferase activity in a concentration-dependent manner with a maximal effect at a concentration of 275 µM. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different brain parts when conjugated to glucose-based carbon nanosphere (CSP).
S7088	UNC1215	UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and K_d of 120 nM, 50-fold selective versus other members of the human MBT family.	Cell Rep, 2022, 39(12):110994 Cancers (Basel), 2022, 14(19)4883 Cell Death Differ, 2021, 28(8):2536-2551
S8889	MZ-1	MZ-1 is a PROTAC degrader of bromodomain-containing protein 4 (BRD4). MZ-1 binds to the Brd bromodomain with Kd of 62 nM, 60 nM, 21 nM, 13 nM, 39 nM and 15 nM for Brd2^BD1, Brd2^BD2, Brd3^BD1, Brd3^BD2, Brd4^BD1 and Brd4^BD2.	Antiviral Res, 2023, 211:105552 Int Immunopharmacol, 2023, 117:109929 Cancers (Basel), 2021, 13(16)4118
E1932^New	DW71177	DW71177 is a potent BD1-Selective inhibitor of BET. DW71177 selectively interacts with BD1 and exhibits strong antileukemic activity. DW71177 can also be used in the study of acute myeloid leukemia.
S8625^New	GNE-049	GNE-049 is a highly potent and selective inhibitor of CBP. It exhibits an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also effectively inhibits BRET and BRD4 with IC50 values of 12 nM and 4200 nM, respectively.
E1683^New	DN02	DN02 is a selective probe of BRD8 bromodomain family. It exhibits potency against BRD8(1) with a Kd of 32 nM, and interestingly, demonstrated this activity to be selective over BRD8's second bromodomain (BRD8(2) with a Kd of >1000 nM)
E1859^New	FHD-609	FHD-609 acts as a selective inhibitor and degrader of BRD9 protein (bromodomain-containing protein 9). FHD-609 targets ncBAF and can be used in research of various cancers involving mutations in a BAF complex subunit.
S7615^New	MS417	MS417 (GTPL7512) is a selective inhibitor of BET-specific BRD4. MS417 binds to BRD4-BD1 and BRD4-BD2 with IC50 values of 30 nM and 46 nM and Kd values of 36.1 nM, and 25.4 nM, respectively. MS417 effectively blocks BRD4 binding to the acetylated NF-κB and attenuates NF-κB transcriptional activation of proinflammatory genes in kidney cells treated with TNFα.
E1664^New	GNE-987	GNE-987 is a BRD4-degradating PROTAC consisting of BRD4B1 and BRD4B2 (BRD4 bromodomains 1 and 2) and the VHL E3-ubiquitin ligase. It exhibits BRD4 degradation activity with DC50 of 0.03 nM for the EOL-1 AML cell line. GNE-987 inhibits cell proliferation and induces apoptosis by promoting the rapid and sustained degradation of BRD4 and inhibiting its downstream targets. It also demonstrates potent antitumor activity in AML cell lines.
E4609^New	Amredobresib	Amredobresib (BI894999) is an oral inhibitor of BET, which acts as an acetyl-lysine mimic. It prevents the bromodomains BRD4-BD1 and BRD4-BD2 from binding to acetylated histones, with an IC50 of 5 nM for BRD4-BD1 and 41 nM for BRD4-BD2.
S2966^New	TTK21	TTK21 is an activator of the histone acetyltransferases CBP/p300. It activates CBP/p300 histone acetyltransferase activity in a concentration-dependent manner with a maximal effect at a concentration of 275 µM. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different brain parts when conjugated to glucose-based carbon nanosphere (CSP).
E1711^New	FHT-1015	FHT-1015 is a potent, small-molecule, allosteric inhibitor of SMARCA4/SMARCA2 ATPase with IC50 values ≤10 nM. FHT-1205 decreases PD1+TIM3+ cells and cytokine expression in vivo.

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