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BRD4 BD1 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (4) c-Myc (1) Caspase (1) CDK (1) Epigenetic Reader Domain (60) Histone Acetyltransferase (2) HIV (2) Ligands for Target Protein for PROTAC (1) p38 MAPK (1) PI3K (1) Polo-like Kinase (PLK) (1) PROTACs (2)
By Research Areas:	Cancer (50) Cardiovascular Disease (2) Infection (3) Inflammation/Immunology (20)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-145310

ZL0590	Epigenetic Reader Domain	Inflammation/Immunology
ZL0590 is a potent, orally active **BRD4 BD1**-selective inhibitor with an IC₅₀ of 90 nM for human BRD4 BD1. ZL0590 exhibits significant anti-inflammatory activities .

HY-151594

iBRD4-BD1	Epigenetic Reader Domain	Inflammation/Immunology Cancer
iBRD4-BD1 is selective BRD4 bromodomain inhibitor. iBRD4-BD1 has inhibition activity for BRD4 bromodomain with an IC₅₀ value of 12 nM. iBRD4-BD1 can be used for the research of inflammation and oncology .

HY-W265951

3-Methylcarbostyril	Epigenetic Reader Domain	Cancer
3-Methylcarbostyril (compound 5) is a **BRD4 BD1** inhibitor with a pIC₅₀ of 4.4 .

HY-163413

BRD4-BD1-IN-3	Epigenetic Reader Domain	Inflammation/Immunology
BRD4-BD1-IN-3 (Compound 4g) is a *BRD4-BD1* inhibitor. BRD4-BD1-IN-3 can be used for research of inflammatory disease .

HY-143299

BRD4-BD1-IN-1	Epigenetic Reader Domain	Cancer
BRD4-BD1-IN-1 (Compound 9a) is a *BRD4-BD1* inhibitor with an IC₅₀ of 38.20 μM .

HY-143300

BRD4-BD1-IN-2	Epigenetic Reader Domain	Cardiovascular Disease Cancer
BRD4-BD1-IN-2 is a selective *BRD4-BD1* inhibitor, with an IC₅₀ of 2.51 µM (20-times greater than that of BD2). BRD4-BD1-IN-2 can be used in studies of cancer and cardiovascular diseases .

HY-142674

BRD4-BD1/2-IN-1	Epigenetic Reader Domain	Cancer
BRD4-BD1/2-IN-1 is a potent *BRD4* inhibitor with IC₅₀s of <100 nM for BRD4 BD-1 and BRD4 BD-2, respectively (US20150148375A1, compound 5) .

HY-149519

BRD4 Inhibitor-28	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-28 (Compound 18) is an orally active *BRD4* Inhibitor. BRD4 Inhibitor-28 inhibits BRD40-BD1, BRD40-BD2 with IC₅₀s of 15, 55 nM. BRD4 Inhibitor-28 also inhibits BRD2-BD1, BRD3-BD1, BRDT-BD1 with IC₅₀s of 19, 25, 68 nM. BRD4 Inhibitor-28 has anti-melanoma activity .

HY-142675

BRD4-BD1/2-IN-2	Epigenetic Reader Domain	Cancer
BRD4-BD1/2-IN-2 is a potent BRD4 BD2 inhibitor with IC₅₀s of <0.5 nM and <300 nM for BRD4 BD2 and BRD4 BD1, respectively (WO2021233371A1, compound 2) .

HY-102044

BET-IN-2	Epigenetic Reader Domain	Cancer
BET-IN-2 is a BET inhibitor with an IC₅₀ of 52 nM for BRD4-BD1.

HY-151594A

iBRD4-BD1 diTFA	Epigenetic Reader Domain	Inflammation/Immunology Cancer
iBRD4-BD1 diTFA is selective BRD4 bromodomain inhibitor. iBRD4-BD1 diTFA has inhibition activity for BRD4 bromodomain with an IC₅₀ value of 12 nM. iBRD4-BD1 diTFA can be used for the research of inflammation and oncology .

HY-160558

PLK1/BRD4-IN-3	Epigenetic Reader Domain Polo-like Kinase (PLK)	Cancer
PLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). PLK1/BRD4-IN-3 inhibits BRD4-BD1, PLK1 and BRDT-BD1, with IC₅₀s of 0.059, 0.127 and 0.245 μM, respectively .

HY-146739

BRD4 Inhibitor-19	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-19 is a BET* inhibitor* with an IC₅₀ of 55 nM for BRD4-BD1. BRD4 Inhibitor-19 can be used for multiple myeloma research .

HY-168628

BET-IN-27	Epigenetic Reader Domain	Cancer
BET-IN-27 (compound 6C) is an oral BET inhibitor with the IC₅₀ values of 3.3 nM (BRD4-BD2)、3.4 nM (BRD4-BD1)、4.1 nM (BRD2-BD1)、20.4 nM (BRD3-BD1) and 42.0 nM (BRDT-BD1), respectively. BET-IN-27 shows anti-proliferative activity .

HY-120000

MS402 1 Publications Verification	Epigenetic Reader Domain	Inflammation/Immunology Cancer
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. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice .

HY-147573

BRD4 Inhibitor-23	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-23 is a potent and orally active *BRD4* inhibitor with IC₅₀s of 6.21 nM and 1.44 nM for BRD4 BD-1 and BRD4 BD-2, respectively (WO2022033542A1; Example 1) .

HY-117491

BRD4 Inhibitor-10	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-10 is a potent *BRD4-BD1* inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC₅₀ of 8 nM .

HY-112149

ZL0420	Epigenetic Reader Domain	Inflammation/Immunology
ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC₅₀ values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.

HY-136570A

GSK778 hydrochloride iBET-BD1 hydrochloride	Apoptosis Epigenetic Reader Domain	Inflammation/Immunology Cancer
GSK778 (iBET-BD1) hydrochloride 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-155078

BRD4 Inhibitor-27	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-27 (compound 6) is a *BRD4* inhibitor with IC₅₀ of 9.6 and 11.3 μM for **BRD4 BD1** and BRD4 BD2, respectively. BRD4 Inhibitor-27 has the potential to study cancer .

HY-149098

SJ1461	Epigenetic Reader Domain	Cancer
SJ1461 is a potent and orally active BET inhibitor. SJ1461 inhibits BRD2 (BD1), and BRD2 (BD2), **BRD4 (BD1)*, and BRD4* (BD2) with IC₅₀ values of 1.6 nM, 0.1 nM, 6.5 nM, and 0.2 nM, respectively .

HY-129201

ZEN-2759	Epigenetic Reader Domain	Cancer
ZEN-2759 is a potent BET (Bromodomain and Extra-Terminal Domain) inhibitor, with IC₅₀ values of 0.23, 0.08 and 0.28 μM for *BRD4(BD1), BRD4(BD2), and BRD4(BD1BD2)*, respectively .

HY-111977

ZEN-3219	Epigenetic Reader Domain	Cancer
ZEN-3219 is a BET inhibitor with IC₅₀s of 0.48, 0.16 and 0.47 μM for *BRD4(BD1), BRD4(BD2)* and *BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4* .

HY-111979

ZEN-3411	Epigenetic Reader Domain	Cancer
ZEN-3411 is a BET inhibitor with IC₅₀s of 0.05, 0.05 and 0.06 μM for *BRD4(BD1), BRD4(BD2)* and *BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTACs to induce degradation of BRD4* .

HY-160634

BRD4 Inhibitor-31	Epigenetic Reader Domain	Infection Inflammation/Immunology Cancer
BRD4 Inhibitor-31 (Example 136) is a *BRD4* inhibitor (K_is: 0.234 μM and 0.295 μM for BRD4 BD1 and BRD4 BD2 respectively). BRD4 Inhibitor-31 can be used for research of inflammatory diseases, cancer, and AIDS .

HY-111978

ZEN-3862	Epigenetic Reader Domain	Cancer
ZEN-3862 is a BET inhibitor with IC₅₀s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively. ZEN-3862 can be used to form PROTACs to induce degradation of BRD4 .

HY-136570

GSK778 iBET-BD1	Epigenetic Reader Domain Apoptosis	Inflammation/Immunology Cancer
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-125232

MS645	Epigenetic Reader Domain	Cancer
MS645 is a bivalent BET bromodomains (BrD) inhibitor with a K_i of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells .

HY-111139

MS417 4 Publications Verification GTPL7512	Epigenetic Reader Domain HIV	Infection Inflammation/Immunology
MS417 is a selective BET-specific *BRD4* inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC₅₀s of 30, 46 nM and K_ds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC₅₀, 32.7 μM).

HY-152209

BRD4 Inhibitor-26	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-26 is a bromodomain protein 4 (BRD4) inhibitor/nitric oxide-donator. BRD4 Inhibitor-26 inhibits BRD4 (BD1) and BRD4 (BD2) with IC₅₀ values of 0.82 μM and 1.94 μM, respectively. BRD4 Inhibitor-26 can be used for the research of ovarian cancer .

HY-153945

BET-IN-15	Epigenetic Reader Domain	Cancer
BET-IN-15 (compound 1) is a potent and orally active BET inhibitor with IC₅₀ values of 0.64, 0.25 nM for BRD4-BD1, BRD4-BD2, respectively. BET-IN-15 shows antiproliferative activity .

HY-130622

LT052	Epigenetic Reader Domain	Inflammation/Immunology
LT052 is a highly selective BET BD1 inhibitor with an IC₅₀ of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC₅₀=12.130 μM). LT052 has anti-inflammatory?activity and can be used for acute gout arthritis research .

HY-112150

ZL0454	Epigenetic Reader Domain	Inflammation/Immunology
ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC₅₀ of 49 and 32 nM for BD1 and BD2.

HY-151972

BRD4 Inhibitor-25	Epigenetic Reader Domain	Cardiovascular Disease Inflammation/Immunology Cancer
BRD4 Inhibitor-25 is a *BRD4* inhibitor with IC₅₀s of 0.82 μM, 1.94 μM for BD1 and BD2 domains of BRD4. BRD4 Inhibitor-25 induces apoptotic and autophagy cell death in ovarian cancer cells. BRD4 Inhibitor-25 can be used in the research of cancers, cardiovascular, neuromuscular and inflammatory disorders.

HY-146208

BRD4 Inhibitor-20	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC₅₀ values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer .

HY-12863

Pelabresib CPI-0610	Epigenetic Reader Domain	Cancer
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-19760

I-BET282	Epigenetic Reader Domain	Inflammation/Immunology
I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC₅₀s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD) .

HY-160557

PLK1/BRD4-IN-2	Epigenetic Reader Domain	Cancer
PLK1/BRD4-IN-2 (compound 15) is a BI-2536 (HY-50698) analog and dual inhibitor that targets both Polo-like kinase 1 (PLK1) and BRD4bromodomain (BRD4-BD1 IC₅₀=28 nM, PLK1 IC₅₀=40 nM) .

HY-146741

SDR-04	Epigenetic Reader Domain	Cancer
SDR-04 is a BET* inhibitor* and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation .

HY-114204

GSK8814	Epigenetic Reader Domain	Cancer
GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pK_d=8.1 and a pK_i=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC₅₀s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1 .

HY-112610

CF53	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
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. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo .

HY-19760B

I-BET282E	Epigenetic Reader Domain	Inflammation/Immunology
I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC₅₀s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD) .

HY-112429

HJB97 2 Publications Verification	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
HJB97 is a high-affinity BET inhibitor with K_i values 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), and 1.0 nM (BRD4* BD2) . HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity . HJB97 can be used for the synthesis of BETd-260 (HY-101519).

HY-112149A

(E/Z)-ZL0420	Epigenetic Reader Domain	Inflammation/Immunology Cancer
(E/Z)-ZL0420 is a racemic compound of (Z)-ZL0420 and (E)-ZL0420 isomers. (E)-ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC₅₀ values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 .

HY-124596

CD161 NKR-P1A	Epigenetic Reader Domain	Cancer
CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC₅₀s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity .

HY-153241

GSK737	Epigenetic Reader Domain	Cancer
GSK737 is a BRD4 *BD1* and BD2 inhibitor, with pIC₅₀ values of 5.3 and 7.3 respectively. GSK737 has low clearance and good solubility and permeability in rat .

HY-126325

BY27	Epigenetic Reader Domain	Cancer
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. Anti-cancer activity .

HY-100482

CPI-637 Maximum Cited Publications 11 Publications Verification	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
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-136794

SB-284851-BT	p38 MAPK Epigenetic Reader Domain	Inflammation/Immunology Cancer
SB-284851-BT is an inhibitor of *BRD4/p38α/BRDT. SB-284851-BT inhibits* *BRD4-BD1* (IC₅₀=1.7 µM), p38α (K_d=0.47 nM), BRDT (1) (IC₅₀=18 µM) and *BRD4* (1)(IC₅₀=3.7 µM). SB-284851-BT reduces IL-8 production by inhibiting p38α, as well as inhibiting BRD4 to down-regulates c-Myc and NF-κB gene pathways in cancer. SB-284851-BT can combined with the bromine domain and extra terminal (BET) .

HY-131203

PROTAC BRD4 Degrader-6	PROTACs Epigenetic Reader Domain Apoptosis c-Myc Caspase	Cancer
PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule *BRD4*PROTAC degrader with IC₅₀ value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research (Pink: Mivebresib (HY-100015); Black: linker, Azido-PEG1-CH2CO2H (HY-108369); Blue: Lenalidomide (HY-A0003)) .

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BRD4 BD1 inhibitor

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