Catalog

Epigenetic Reader Domain Epigenetic Reader Domain

Inhibitors

Cat.No.	Name	Information
M9238	dBET6	dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM.
M9237	dBET1	dBET1 is a potent BRD4 protein degrader with an EC50 of 430 nM.
M9218	ABBV-744	ABBV-744 is a BDII-selective BET bromodomain inhibitor that is used in the research of AML and metastic castration-resistant prostate cancer.
M9152	CPI-637	CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.
M9146	GSK1324726A	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.
M9144	PFI-3	PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains with a Kd of 89 nM.
M9141	SGC-CBP30	SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively.
M9105	ARV-771	ARV-771 is a small-molecule pan-BET degrader with Kd values of 4.7, 7.6, 7.6 nM against BRD2, BRD3 and BRD4, respectively.
M9100	PLX51107	PLX51107 is a potent and selective BET inhibitor, with Kds of 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.
M9026	AZD-5153 HNT salt	AZD-5153 HNT salt is a potent, selective and orally available BET/BRD4 bromodomain inhibitor, disrupts BRD4 with an IC50 of 1.7 nM.
M8931	BI-7273	BI-7273 is a potent and selective BRD9 inhibitor with IC50s of 19 nM and 117 nM for BRD9 and BRD7, respectively.
M6206	ARV-825	ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 shows affinity to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.
M6118	666-15	666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM.
M6096	JQ-1 carboxylic acid	(+)-JQ1 carboxylic acid is the carboxylic acid form of (+)-JQ1 for derivative synthesis.
M6083	AZD9496	AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.
M5271	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.
M5258	Mivebresib	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)
M5064	PFI 4	PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.
M4909	GSK2801	GSK2801 is a selective bromodomains BAZ2A/B inhibitor with KD of 257 nM and 136 nM, respectively.
M3526	CPI-203	CPI-203 is a novel potent, selective BET bromodomain inhibitor with IC50 of 37 nM for BRD4.
M3106	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.
M2932	PFI-1	PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM.
M2903	OTX015	OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4.
M2219	RVX-208	RVX-208 is a first-in-class, small molecule inhibitor of BET bromodomain with IC50 of 0.51 μM for BD2.
M2202	CPI-0610	CPI-0610 is a novel BET protein bromodomain inhibitor.
M2190	I-BET-762	I-BET-762 (GSK525762) is a selective small molecule BET inhibitor.
M2167	(+)-JQ1	(+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor.
M2096	GSK1210151A	GSK1210151A (I-BET151) is an inhibitor of the BET family with IC50 of 0.5 μM, 0.25 μM and 0.79 μM for BRD2, BRD3 and BRD4, respectively.

Signaling Pathways

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Epigenetic Reader Domain Epigenetic Reader Domain

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