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BET/BRD4 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (2) Apoptosis (16) Autophagy (2) c-Myc (2) CDK (1) Drug Intermediate (1) Drug Isomer (1) Drug Metabolite (1) E3 Ligase Ligand-Linker Conjugates (1) Epigenetic Reader Domain (95) ERK (1) HDAC (2) Histone Acetyltransferase (2) HIV (2) Interleukin Related (1) Ligands for Target Protein for PROTAC (14) Necroptosis (1) p38 MAPK (1) PD-1/PD-L1 (2) Polo-like Kinase (PLK) (1) PROTACs (6) Reactive Oxygen Species (ROS) (1) Reference Standards (4) STAT (1)
By Research Areas:	Cancer (87) Infection (2) Inflammation/Immunology (16) Neurological Disease (2)
Click Chemistry:	PROTAC Synthesis (1)

Inhibitors & Agonists

Biochemical Assay Reagents

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13030

(+)-JQ-1 Maximum Cited Publications 301 Publications Verification JQ1	Epigenetic Reader Domain Autophagy Ligands for Target Protein for PROTAC	Neurological Disease Cancer
(+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, CNS-penetrant and reversible BET bromodomain inhibitor, with IC₅₀s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)) . (+)-JQ-1 also activates autophagy .

HY-78695

JQ-1 carboxylic acid 5+ Cited Publications	Epigenetic Reader Domain PD-1/PD-L1 Ligands for Target Protein for PROTAC Androgen Receptor	Cancer
JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of *BRD4*.

HY-13235

I-BET151 25+ Cited Publications GSK1210151A	Epigenetic Reader Domain	Cancer
I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits *BRD4, BRD2, and BRD3* with pIC₅₀ of 6.1, 6.3, and 6.6, respectively .

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-100015

Mivebresib 10+ Cited Publications ABBV-075	Epigenetic Reader Domain Apoptosis	Cancer
Mivebresib (ABBV-075) is a potent and orally active *bromodomain and extraterminal domain (BET) bromodomain* inhibitor. Mivebresib binds to *BRD4* with a K_i of 1.5 nM .

HY-136570

GSK778 2 Publications Verification iBET-BD1	Epigenetic Reader Domain Apoptosis	Inflammation/Immunology Cancer
GSK778 (iBET-BD1), a chemical probe, 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-112090

ABBV-744 10+ Cited Publications	Epigenetic Reader Domain HIV	Infection Inflammation/Immunology Cancer
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-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-15846

CPI-203 5+ Cited Publications	Epigenetic Reader Domain Apoptosis	Cancer
CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC₅₀ value of appr 37 nM (BRD4 α-screen assay).

HY-13960

GSK1324726A 5+ Cited Publications I-BET726	Ligands for Target Protein for PROTAC Epigenetic Reader Domain Apoptosis	Cancer
GSK1324726A is a novel, potent, and selective inhibitor of *BET* proteins with high affinity to BRD2 (IC₅₀=41 nM), BRD3 (IC₅₀=31 nM), and *BRD4* (IC₅₀=22 nM).

HY-100653

AZD5153 5 Publications Verification	Epigenetic Reader Domain Apoptosis	Cancer
AZD5153 is a bivalent, selective, and orally active *BET/BRD4* bromodomain inhibitor with an IC₅₀ of value of 5 nM for full-length BRD4 (FL-BRD4). AZD5153 ligates two bromodomains in BRD4 simultaneously. AZD5153 can be used for the study of cancer, such as acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma .

HY-100653A

AZD5153 6-Hydroxy-2-naphthoic acid 5 Publications Verification	Epigenetic Reader Domain	Cancer
AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available *BET/BRD4* bromodomain inhibitor; disrupts BRD4 with an IC₅₀ of 1.7 nM.

HY-111422

PLX51107 4 Publications Verification	Histone Acetyltransferase Epigenetic Reader Domain	Cancer
PLX51107 is a potent and selective *BET* inhibitor, with K_ds 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; PLX51107 also interacts with the bromodomains of CBP and EP300 (K_d, in the 100 nM range).

HY-129939

BET-IN-31	Epigenetic Reader Domain Ligands for Target Protein for PROTAC	Cancer
BET-IN-31 is a potent *BET* inhibitor and a ligand for target *BRD4* protein for PROTACT GNE-987 (HY-129937A) .

HY-114407

TD-428	PROTACs Epigenetic Reader Domain	Cancer
TD-428 is a PROTAC connected by ligands for Cereblon and *BRD4. TD-428 is a highly specific BRD4* degrader with a DC₅₀ of 0.32 nM . TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation .

HY-145550

Amredobresib BI894999	Epigenetic Reader Domain	Cancer
Amredobresib (BI894999) is an orally active *BET* inhibitor. Amredobresib inhibits the binding of *BRD4-BD1* and *BRD4-BD2* bromodomains to acetylated histones with IC₅₀ values of 5 nM and 41 nM, respectively. Amredobresib exhibits anticancer activity against acute myeloid leukemia (AML) and NUT cancer .

HY-16586

PFI-1 4 Publications Verification	Epigenetic Reader Domain Autophagy Apoptosis	Cancer
PFI-1, a chemical probe, is a selective *BET* (bromodomain-containing protein) inhibitor for BRD4 with IC₅₀ of 0.22 μM in a cell-free assay.

HY-107443

I-BET762 carboxylic acid Molibresib carboxylic acid; GSK525762A carboxylic acid; PROTAC BRD4-binding moiety 2	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a *BRD4* inhibitor with a pIC₅₀ of 5.1 .

HY-136571

GSK046 4 Publications Verification iBET-BD2	Epigenetic Reader Domain	Inflammation/Immunology
GSK046 (iBET-BD2), a chemical probe, 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-134463

NHWD-870 1 Publications Verification	Epigenetic Reader Domain Apoptosis	Cancer
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC₅₀=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .

HY-13032B

Molibresib besylate 20+ Cited Publications GSK 525762C; I-BET 762 besylate	Epigenetic Reader Domain ERK	Cancer
Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between *BET* proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors .

HY-120000

MS402 2 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-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-117286

(S)-JQ-35 TEN-010	Epigenetic Reader Domain Apoptosis	Neurological Disease Cancer
(S)-JQ-35 (TEN-010) is an orally active, blood-brain barrier-permeable bromodomain inhibitor that selectively targets the bromodomain and extra-terminal domain (BET) protein family (BRD4, BRD3, BRD2 and BRDT). (S)-JQ-35 blocks the activation of Myc gene expression by BRD4, thereby inhibiting cancer cell proliferation and promoting cancer cell apoptosis. (S)-JQ-35 can be used in research related to NUT midline carcinoma and neuroblastoma .

HY-125232

MS645 1 Publications Verification	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-131061

BET bromodomain inhibitor 1	Epigenetic Reader Domain	Cancer
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. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (K_d values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity .

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-103036

BET bromodomain-IN-5	Epigenetic Reader Domain Apoptosis	Cancer
BET bromodomain-IN-5 is an orally active *BET* inhibitor with an IC₅₀ of 14 nM against *BRD4* (1). BET bromodomain-IN-5 can inhibit the proliferation of tumor cells and induce cell cycle arrest and apoptosis. BET bromodomain-IN-5 can be used in the research of tumors .

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-163729

I-BET787	Epigenetic Reader Domain	Inflammation/Immunology Cancer
I-BET787 is a orally active BET bromine domain inhibitor with pIC₅₀s of 7.1 and 5.9 for BRD4 BD1 and BRD4 BD2, respectively. I-BET787 has anti-inflammatory activity in mice .

HY-124596

CD161	Epigenetic Reader Domain	Cancer
CD161 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-111502

Y06036 1 Publications Verification	Epigenetic Reader Domain	Cancer
Y06036 is a potent and selective *BET* inhibitor, which binds to the *BRD4(1)* bromodomain with K_d value of 82 nM . Antitumor activity .

HY-110215

XD14	Epigenetic Reader Domain	Cancer
XD14 is a potent *BET* inhibitor with antitumor effect. It binds to BRD2, BRD3, and BRD4 with K_ds of 170, 380, and 160 nM, respectively .

HY-130622

LT052 2 Publications Verification	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-142520

I-BET567	Epigenetic Reader Domain	Inflammation/Immunology Cancer
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. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation .

HY-138563

GSK973	Epigenetic Reader Domain	Cancer
GSK973, a chemical probe, 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. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC₅₀=7.4~7.8; pK_d=8.3~8.5) .

HY-158764

PROTAC BET Degrader-12	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BET Degrader-12 (Compound 8b) is a PROTAC degrader for bromodomain and extra-terminal domain (BET)-containing proteins, which degrades the BRD3 and *BRD4* in a DCAF11-dependent manner. PROTAC BET Degrader-12 inhibits cell viability of KBM7 with a DC₅₀ of 305.2 nM

HY-147046

ET-JQ1-OH	Epigenetic Reader Domain Ligands for Target Protein for PROTAC	Cancer
ET-JQ1-OH is an allele-specific BET inhibitor. ET-JQ1-OH can serve as a Ligand for Target Protein for PROTAC, and is used for the development and design of PROTAC Brd4 degraders, such as AB3145 (HY-180923).

HY-114504

RVX-297	Epigenetic Reader Domain	Inflammation/Immunology
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC₅₀s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models .

HY-111916

ODM-207 BET-IN-4	Epigenetic Reader Domain	Cancer
ODM-207 (BET-IN-4) is a potent *BET* bromodomain protein (BRD4) inhibitor, with an IC₅₀ of ≤ 1 μM .

HY-100696

PNZ5	Epigenetic Reader Domain	Cancer
PNZ5 is a potent and isoxazole-based *pan-BET* inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a K_D of 5.43 nM for BRD4(1) .

HY-44103

Desmethyl-QCA276 PROTAC BRD4-binding moiety 4	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade *BET. QCA276 is a BET* inhibitor with an IC₅₀ of 10 nM, and with a K_i of 2.3 nM . Desmethyl-QCA276 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-125236

ZEN-3694 1 Publications Verification BET-IN-19	Epigenetic Reader Domain	Cancer
ZEN-3694 (Compound 146) is a *BET* inhibitor. ZEN-3694 inhibits hlL-6 mRNA transcription (IC₅₀ ≤0.3 uM), and c-myc activity in human AML MV4-11 cell (IC₅₀ ≤0.3 uM). ZEN-3694 inhibits tetra-acetylated histone H4 binding to BRD4 bromodomain 1 (IC₅₀ ≤0.3 uM) .

HY-112316B

(Rac)-BAY1238097	Epigenetic Reader Domain	Cancer
(Rac)-BAY1238097 is a *BET* inhibitor, with an IC₅₀ of 1.02 μM for BRD4. Used in cancer research .

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-130612

PROTAC BRD2/BRD4 degrader-1	Epigenetic Reader Domain PROTACs	Cancer
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. PROTAC BRD2/BRD4* degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. PROTAC BRD2/BRD4 degrader-1 effectively inhibits solid tumors with low cytotoxic effect .

HY-130813

BET-IN-6	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
BET-IN-6 is a potent and high affnity *BRD2/BRD4* inhibitor. BET-IN-6 is the ligand for target protein BRD2/4, and is used for the systhesis of PROTAC BRD2/BRD4 degrader-1 (HY-130612) .

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-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* .

Cat. No.	Product Name		Classification

HY-44103

Desmethyl-QCA276 PROTAC BRD4-binding moiety 4		PROTAC Synthesis
Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade *BET. QCA276 is a BET* inhibitor with an IC₅₀ of 10 nM, and with a K_i of 2.3 nM . Desmethyl-QCA276 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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