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Epigenetic Reader Domain
Isoform-selective Products
Signaling Pathway
Epigenetic Reader Domain Products
- All (89)
- Epigenetic Reader Domain Inhibitors (83)
- Epigenetic Reader Domain Activators (2)
- Epigenetic Reader Domain Antagonist (1)
- Epigenetic Reader Domain Modulator (1)
- New Epigenetic Reader Domain Products
| Catalog No. | Product Name | Information | Product Use Citations | Product Validations |
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| 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. |
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| 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. |
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| 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. |
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| S7152 | C646 | C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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 Kd of 80 nM and 170 nM for ERK5 and BRD4(1), respectively. |
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| 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. |
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| 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. | ||
| 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. |
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| 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. | ||
| 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. |
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| 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. | ||
| 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. | ||
| S7304 | CPI-203 | CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4. | ||
| 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. | ||
| S7315 | PFI-3 | PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains. |
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| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S7088 | UNC1215 | UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and Kd of 120 nM, 50-fold selective versus other members of the human MBT family. | ||
| 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. | ||
| 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. | ||
| 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). | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S7305 | MS436 | MS436 is a selective BET bromodomain inhibitor with Ki of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively. |
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| 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. | ||
| S7231 | GSK2801 | GSK2801 is a selective bromodomains BAZ2A/B inhibitor with KD of 257 nM and 136 nM, respectively. | ||
| 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. | ||
| 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 Brd2BD1, Brd2BD2, Brd3BD1, Brd3BD2, Brd4BD1 and Brd4BD2. | ||
| 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. | ||
| 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. | ||
| S7681 | OF-1 | OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S7906 | PFI-4 | PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM. | ||
| 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. | ||
| 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. | ||
| S0137 | dBET57 | dBET57 is a novel, potent and selective degrader of BRD4BD1 based on the PROTAC technology with DC50/5h of 500 nM. dBET57 is inactive on BRD4BD2. | ||
| 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. | ||
| 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. |
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| 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. | ||
| 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. | ||
| E1932New | 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. | ||
| S8625New | 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. | ||
| E1683New | 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. | ||
| E1859New | 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| E4609New | 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 BRD2BD2, BRD3BD2, BRD4BD2 and BRDTBD2, 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. |
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| S2966New | 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. | ||
| E1711New | 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. |
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| 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. |
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| 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. |
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| S7152 | C646 | C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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 Kd of 80 nM and 170 nM for ERK5 and BRD4(1), respectively. |
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| 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. |
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| 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. | ||
| 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. |
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| 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. | ||
| 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. |
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| 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. | ||
| 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. | ||
| S7304 | CPI-203 | CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4. | ||
| 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. | ||
| S7315 | PFI-3 | PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains. |
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| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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). | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S7305 | MS436 | MS436 is a selective BET bromodomain inhibitor with Ki of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively. |
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| 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. | ||
| S7231 | GSK2801 | GSK2801 is a selective bromodomains BAZ2A/B inhibitor with KD of 257 nM and 136 nM, respectively. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S7681 | OF-1 | OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S7906 | PFI-4 | PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM. | ||
| 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. | ||
| 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. | ||
| S0137 | dBET57 | dBET57 is a novel, potent and selective degrader of BRD4BD1 based on the PROTAC technology with DC50/5h of 500 nM. dBET57 is inactive on BRD4BD2. | ||
| 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. | ||
| 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. |
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| 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. | ||
| 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. | ||
| E1932New | 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. | ||
| S8625New | 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. | ||
| E1859New | 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| E4609New | 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 BRD2BD2, BRD3BD2, BRD4BD2 and BRDTBD2, 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. |
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| 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. | ||
| E1711New | 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. | ||
| S2966New | 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 Kd of 120 nM, 50-fold selective versus other members of the human MBT family. | ||
| 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 Brd2BD1, Brd2BD2, Brd3BD1, Brd3BD2, Brd4BD1 and Brd4BD2. | ||
| E1932New | 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. | ||
| S8625New | 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. | ||
| E1683New | 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) | ||
| E1859New | 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. | ||
| E4609New | 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. | ||
| S2966New | 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). | ||
| E1711New | 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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