bromodomain Selective Inhibitors | Antagonists

Catalog No.	Product Name	Information	Selective / Pan	IC50 / Ki
S2943	BRD9539	BRD9539 is a histone methyltransferase G9a inhibitor, which also inhibits PRC2 activity.	Selective
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.	Selective	L3MBTL3, IC50: 40 nM; L3MBTL3, Kd: 120 nM; L3MBTL3- D274A, IC50: 3.5 μM
S7315	PFI-3	PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.	Selective	SMARCA2A, Kd: 110 nM; SMARCA4, Kd: 55 nM; PB1(5) bromodomains, : ; SMARCA2B, Kd: 72 nM
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.	Selective	CREB, IC50: 81 nM
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.	Selective	PRC2, Kd: 114 nM; EED, Kd: 82 nM
S7231	GSK2801	GSK2801 is a selective bromodomains BAZ2A/B inhibitor with K_D of 257 nM and 136 nM, respectively.	Selective	BAZ2A, Kd: 257 nM; BAZ2B, Kd: 136 nM
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.	Selective	EED, IC50: 247 nM
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.	Selective	L3MBTL1, Kd: 3.9 μM
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.	Selective	L3MBTL1, IC50: 6 μM; L3MBTL3, IC50: 35 μM; L3MBTL4, IC50: 69 μM
S8409	KG-501 (2-naphthol-AS-E-phosphate)	KG-501 (2-naphthol-AS-E-phosphate) 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.	Selective
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.	Pan	CECR2, IC50: 17 nM
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.	Pan	CECR2, Kd: 77 nM