BRD2 Inhibitor

BRD2 Inhibitors (21):

Cat. No.	Product Name	Effect	Purity

HY-100972

ARV-771	Inhibitor	99.02%
ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with K_ds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.

HY-112090

ABBV-744	Inhibitor	99.97%
ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC₅₀ values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT.

HY-136570

GSK778	Inhibitor	99.25%
GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC₅₀s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively.

HY-136571

GSK046	Inhibitor	98.15%
GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC₅₀s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively.

HY-101519

BETd-260	Inhibitor	99.59%
BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line.

HY-152213

BET-IN-13	Inhibitor
BET-IN-13 is a potent BET inhibitor with an IC₅₀ value of 1.6 nM.

HY-151972

BRD4 Inhibitor-25	Inhibitor
BRD4 Inhibitor-25 is a BRD4 inhibitor with IC₅₀s of 0.82 μM, 1.94 μM for BD1 and BD2 domains of BRD4.

HY-141438

SIM1	Inhibitor	99.72%
SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC₅₀=1.1 nM; Kd=186 nM).

HY-120000

MS402	Inhibitor	99.62%
MS402 is a BD1-selective BET BrD inhibitor with K_is of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively.

HY-112429

HJB97	Inhibitor	98.24%
HJB97 is a high-affinity BET inhibitor with K_is of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively.

HY-114416

GS-626510	Inhibitor	99.86%
GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with K_d values of 0.59-3.2 nM for BRD2/3/4, with IC₅₀ values of 83 nM and 78 nM foe BD1 and BD2, respectively.

HY-112610

CF53	Inhibitor	99.78%
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K_i of <1 nM, K_d of 2.2 nM and an IC₅₀ of 2 nM for BRD4 BD1.

HY-114504

RVX-297	Inhibitor
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2.

HY-145264

OARV-771	Inhibitor	98.33%
OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability.

HY-142520

I-BET567	Inhibitor	99.68%
I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC₅₀s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively.

HY-131061

BET bromodomain inhibitor 1	Inhibitor	99.91%
BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC₅₀ of 2.6 nM for BRD4.

HY-130612

PROTAC BRD2/BRD4 degrader-1	Inhibitor
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET.

HY-126325

BY27	Inhibitor
BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT.

HY-138563

GSK973	Inhibitor
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC₅₀ of 7.8 and a pK_d of 8.7 for BRD4 BD2.

HY-110215

XD14	Inhibitor
XD14 is a potent BET inhibitor with antitumor effect.

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