BRD4 Inhibitor

BRD4 Inhibitors (97):

Cat. No.	Product Name	Effect	Purity

HY-100972

ARV-771	Inhibitor	99.87%
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-101838

dBET1	Inhibitor	99.24%
dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC₅₀ of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker.

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. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability.

HY-136570

GSK778	Inhibitor	98.93%
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. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.

HY-122826

ZXH-3-26	Inhibitor	98.61%
ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC_50/5h of 5 nM. The DC_50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM.

HY-12863

Pelabresib	Inhibitor	99.95%
Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active BET inhibitor. Pelabresib inhibits BRD4-BD1 with an IC₅₀ of 39 nM, and with an EC₅₀ value of 0.18 μM for MYC.

HY-148864A

(Z)-JQ1-TCO	Inhibitor
JQ1-TCO (JQ1-trans-cyclooctene) is a derivative of JQ1 (HY-13030), an inhibitor of BET. JQ1-TCO is suitable for click chemistry and can be used as molecular probes in vitro and in vivo.

HY-14443

XMD8-92	Inhibitor	99.67%
XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with K_ds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with K_ds of 190, 600 and 890 nM, respectively. Anti-cancer activity.

HY-100482

CPI-637	Inhibitor	99.94%
CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC₅₀ values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC₅₀ of 0.3 μM for CBP.

HY-136571

GSK046	Inhibitor	99.65%
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. GSK046 has immunomodulatory activity.

HY-123941

FKBP12 PROTAC dTAG-7	Inhibitor	99.88%
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12^F36V with expression of FKBP12^F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.

HY-114305

A1874	Inhibitor	99.28%
A1874 is a nutlin-based (MDM2 ligand) and BRD4-degrading PROTAC with a DC₅₀ of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.

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. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.

HY-103632

PROTAC BRD9 Degrader-1	Inhibitor	98.30%
PROTAC BRD9 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD9 (IC₅₀=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology.

HY-19999A

PF-CBP1 hydrochloride	Inhibitor	99.99%
PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with IC₅₀ of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1β, IL-6 and IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates RGS4 expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al.

HY-129937A

GNE-987	Inhibitor	99.91%
GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC₅₀=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC₅₀=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).

HY-123844

dBET57	Inhibitor	99.66%
dBET57 is a potent and selective degrader of BRD4_BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4^Cereblon E3 ubiquitin ligase, with a DC_50/5h of 500 nM for BRD4_BD1, and is inactive on BRD4_BD2.

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). SIM1 shows sustained anti-cancer activity.

HY-120028

GNE-207	Inhibitor
GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC₅₀ of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC₅₀ of 18 nM for MYC expression in MV-4-11 cells.

HY-133737

PROTAC BRD4 Degrader-5	Inhibitor	99.93%
PROTAC BRD4 Degrader-5 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-5 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines.

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