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Results for "

BET inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (1) Antibiotic (1) Apoptosis (14) ATP-binding cassette (ABC) transporters (1) Aurora Kinase (1) Autophagy (2) Bacterial (1) c-Myc (1) CDK (1) Drug Metabolite (1) Epigenetic Reader Domain (146) FLT3 (1) Fungal (1) HDAC (2) Hedgehog (1) Histone Acetyltransferase (2) HIV (4) HSP (1) IFNAR (2) JAK (1) Ligands for E3 Ligase (1) Ligands for Target Protein for PROTAC (10) p38 MAPK (1) PD-1/PD-L1 (1) Polo-like Kinase (PLK) (1) PROTACs (7) SNIPERs (1) STAT (2)
By Research Areas:	Cancer (130) Cardiovascular Disease (1) Infection (6) Inflammation/Immunology (29) Metabolic Disease (1) Neurological Disease (4)
Click Chemistry:	Alkynes (1)

156

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-103036

**BET bromodomain inhibitor**	Epigenetic Reader Domain	Cancer
BET bromodomain inhibitor is a potent *BET* inhibitor extracted from patent WO/2015/153871A2, compound example 11.

HY-153593

BET bromodomain inhibitor 3	Epigenetic Reader Domain	Cancer
BET bromodomain inhibitor 3 is BET bromodomain inhibitor. BET bromodomain inhibitor 3 has inhibitory effect against BrdT with K_i value of > 40 µM. BET bromodomain inhibitor 3 can be used for the research of contraception, cancer, and heart disease .

HY-157393

BET bromodomain inhibitor 4	Epigenetic Reader Domain	Cancer
BET bromodomain inhibitor 4 (example 7) is an inhibitor of the BET bromodomain domain .

HY-163729

I-BET787	Epigenetic Reader Domain	Inflammation/Immunology
I-BET787 is a *pan-BET* bromine domain inhibitor with oral activity. I-BET787 shows effectiveness in a mouse model of inflammation .

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-146709

BET bromodomain inhibitor 2	Epigenetic Reader Domain	Cancer
BET bromodomain inhibitor 2 is a potent BET bromodomain inhibitor with an IC₅₀ of 14.1 µM .

HY-150516S

BET-IN-12	Epigenetic Reader Domain	Cancer
BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4[1].

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-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-116588

FT001	Epigenetic Reader Domain	Cancer
FT001 is an orally active and selective *BET* inhibitor. FT001 has potent anti-proliferative effects against MV-4-11. FT001 can be used for research of cancer .

HY-12421B

BET-BAY 002 (S enantiomer)	Epigenetic Reader Domain	Cancer
BET-BAY 002 S enantiomer is the S-enantiomer of BET-BAY 002. BET-BAY 002 is a *BET* inhibitor.

HY-155809

BET-IN-17	Epigenetic Reader Domain	Cancer
BET-IN-17 (compound 16) is a pan-inhibitor of BET with pIC₅₀s of 7.8 and 7.6 for BET BD1 and BET BD2, respectively .

HY-43723

PROTAC BET-binding moiety 2	Ligands for Target Protein for PROTAC	Cancer
PROTAC BET-binding moiety 2 is an inhibitor of BET bromodomain .

HY-142265

NVS-BET-1	Epigenetic Reader Domain	Others
NVS-BET-1 is a BET bromodomain inhibitor that regulates keratinocyte plasticity.

HY-153226

BET-IN-14	Epigenetic Reader Domain	Cancer
BET-IN-14 is an orally active pan *BET* inhibitor (IC₅₀: 5.35 nM). BET-IN-14 has anti-cancer activity .

HY-12421

BET-BAY 002	Epigenetic Reader Domain	Cancer
BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model.

HY-150268

BET-IN-16	Epigenetic Reader Domain	Cancer
BET-IN-16 (Comp I) is a *BET* inhibitor. BET-IN-16 shows anticancer activity. BET-IN-16 inhibits prostate cancer cell growth, with IC₅₀ values of 0.043 and 0.034 μM against LNCaP and 22Rv1 cells, respectively .

HY-160499

*BRD4 Inhibitor-30*	Epigenetic Reader Domain	Cancer
BRD4 inhibitor-30 (Compound 1) is a BRD4 inhibitor with a IC₅₀ value of 415 nM .

HY-107443A

(R)-I-BET762 carboxylic acid (R)-Molibresib carboxylic acid; (R)-GSK525762A carboxylic acid; (R)-PROTAC BRD4-binding moiety 2	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
(R)-I-BET762 carboxylic acid, the R-enantiomer of I-BET762 carboxylic acid (HY-107443). I-BET762 carboxylic acid is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid is a BRD4 inhibitor with a pIC₅₀ value of 5.1 .

HY-146292

BET-IN-8	Epigenetic Reader Domain	Infection
BET-IN-8 (Compound 27) is a potent inhibitor of *BET* with a K_i and K_d of 0.83 and 0.571 μM, respectively. BET-IN-8 ameliorates LPS-induced sepsis in vivo. BET-IN-8 has the potential for the research of sepsis .

HY-147572

BET-IN-10	Epigenetic Reader Domain	Cancer
BET-IN-10 is a *BET* inhibitor with anticancer effects. BET-IN-10 inhibits the cell growth of MV4-11 cells with an IC₅₀ of 26.5 nM (WO2022012456A1; example 6) .

HY-146291

BET-IN-7	Epigenetic Reader Domain	Infection
BET-IN-7 (Compound 1) is a potent inhibitor of *BET* with a K_i and K_d of 12.27 and 89.3 μM, respectively. BET-IN-7 has the potential for the research of sepsis .

HY-107451

PROTAC BET-binding moiety 1	Ligands for Target Protein for PROTAC	Cancer
PROTAC BET-binding moiety 1 is a key intermediate for the synthesis of high-affinity BET inhibitors .

HY-115727

BET-IN-1	Epigenetic Reader Domain	Others
BET-IN-1 is a potent *BET* inhibitor that has excellent brain penetration and reasonable metabolic stability.

HY-157430

BET-IN-21	Epigenetic Reader Domain	Neurological Disease
BET-IN-21 (compound 16) is a blood-brain barrier-permeable extra terminal domain (BET) inhibitor with the K_i of 230 nM. BET-IN-21 inhibits microglia activation and has ameliorative effects on experimental autoimmune encephalomyelitis mice .

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-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-147571

BET-IN-9	Epigenetic Reader Domain	Cancer
BET-IN-9 is a *BET* inhibitor extracted from patent WO2022012456A1, compound example 1 .

HY-13032

Molibresib 15+ Cited Publications I-BET762; GSK525762; GSK525762A	Epigenetic Reader Domain	Cancer
Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC₅₀ of 32.5-42.5 nM.

HY-160446

BET-IN-24	Epigenetic Reader Domain	Infection Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
Bet-in-24 (example 2) is a bromodomain and extra-terminal (BET) inhibitor. BET-IN-24 can be used in the study of virology, heart failure, inflammation, central nervous system (CNS) diseases and many cancers

HY-152213

BET-IN-13	Epigenetic Reader Domain	Inflammation/Immunology
BET-IN-13 is a potent *BET* inhibitor with an IC₅₀ value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury .

HY-151894

I-BET432	Epigenetic Reader Domain	Cancer
I-BET432 is a *BET* inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC₅₀ values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases .

HY-159602

BET BD2-IN-3	Epigenetic Reader Domain	Cancer
BET BD2-IN-3 (compound I-58) is an inhibitor of BET, targeting the BD2 domain of BET. BET BD2-IN-3 can be radiolabeled with [11C] for positron emission tomography (PET) imaging. BET [11C]BD2-IN-3 showed suitable biodistribution in peripheral organs and tissues in PET applications in mice .

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-13032B

Molibresib besylate 15+ Cited Publications GSK 525762C; I-BET 762 besylate	Epigenetic Reader Domain	Cancer
Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC₅₀ of 32.5-42.5 nM.

HY-125236

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

HY-155680

BET BD2-IN-1	Epigenetic Reader Domain	Inflammation/Immunology
BET BD2-IN-1 (compound 45) is a potent and selective inhibitor of BET BD2 (IC₅₀=1.6 nM). BET BD2-IN-1 inhibits the differentiation of Th17 cells by decreasing the activation of STAT3 and NF-κB. BET BD2-IN-1 is used in psoriasis and inflammatory bowel disease (IBD) research .

HY-112504

INCB054329 2 Publications Verification	Epigenetic Reader Domain	Cancer
INCB054329 is a potent *BET* inhibitor.

HY-112504A

INCB054329 Racemate	Epigenetic Reader Domain	Cancer
INCB054329 Racemate is a *BET* protein inhibitor.

HY-163160

BET-IN-23	Apoptosis Epigenetic Reader Domain	Cancer
Bet-in-23 (Compound 23) is a BD2-selective BET inhibitor with an IC₅₀ of 2.9 nM. BET-IN-23 has anticancer activity and can significantly inhibit the proliferation of acute myeloid leukemia (AML) cell lines by inducing G0/G1 arrest and apoptosis in vitro .

HY-115568

BETd-246 2 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and *BET*, exhibiting superior selectivity, potency and antitumor activity .

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-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-163543

Progranulin modulator-2	Epigenetic Reader Domain	Neurological Disease
Progranulin modulator-2 (compound 18A) is a bromodomain and extra-terminal domain (BET) inhibitor. Progranulin modulator-2 enhances PGRN expression by targeting members of the *BET* protein family. Progranulin modulator-2 can be used to study the role of *BET* protein in neurodevelopment, neuroplasticity and neurodegeneration .

HY-110106

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

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-111485

INCB-057643	Epigenetic Reader Domain Apoptosis	Cancer
INCB-057643 is a novel, orally bioavailable *BET* inhibitor.

HY-132230

GSK040	Epigenetic Reader Domain	Inflammation/Immunology Cancer
GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC₅₀ of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC₅₀=4.6). GSK040 can be used for the research of oncology and immunology diseases .

HY-170812

BET/Aurora kinase-IN-1	Aurora Kinase	Cancer
BET/Aurora kinase-IN-1 (Compound 38) is a dual BET/Aurora kinase inhibitor. BET/Aurora kinase-IN-1 shows antiproliferative activities on diverse cancer cell lines and favorable antitumor efficacy in renal cell cancer and colon cancer xenograft models with tumor growth inhibition (TGI) of 45.99% and 53.06%, respectively .

HY-149735

BET-IN-20	Epigenetic Reader Domain Apoptosis	Cancer
BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC₅₀=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage .

Cat. No.	Product Name

HY-L129

Target Protein Ligand Library

54 compounds

Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.

MCE carefully prepared a unique collection of 54 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-119347

Cirsilineol 3 Publications Verification	Laburnum anagyroides Medic. Structural Classification Monophenols Flavonoids Classification of Application Fields Flavones Source classification Phenols Plants Compositae Inflammation/Immunology Disease Research Fields	IFNAR STAT
Cirsilineol, a natural flavone compound, selectively inhibits IFN-γ/STAT1/T-bet signaling in intestinal CD4 ⁺ T cells. Cirsilineol has potent immunosuppressive and anti-tumor properties. Cirsilineol significantly ameliorates trinitro-benzene sulfonic acid (TNBS)-induced T-cell-mediated experimental colitis in mice .

HY-152245

Physachenolide C	Structural Classification Source classification Physalis chenopodifolia Lam Plants Solanaceae Steroids	Epigenetic Reader Domain
Physachenolide C is a potent and selective *BET* inhibitor that induces apoptosis and arrests the cell cycle in the G0-G1 phase, with antitumor activity .

HY-119347R

Cirsilineol (Standard)	Laburnum anagyroides Medic. Structural Classification Monophenols Flavonoids Flavones Source classification Phenols Plants Compositae	IFNAR STAT
Cirsilineol (Standard) is the analytical standard of Cirsilineol. This product is intended for research and analytical applications. Cirsilineol, a natural flavone compound, selectively inhibits IFN-γ/STAT1/T-bet signaling in intestinal CD4+ T cells. Cirsilineol has potent immunosuppressive and anti-tumor properties. Cirsilineol significantly ameliorates trinitro-benzene sulfonic acid (TNBS)-induced T-cell-mediated experimental colitis in mice .

Cat. No.	Product Name	Chemical Structure

HY-150516S

BET-IN-12
BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4[1].

Cat. No.	Product Name		Classification

HY-112789

(+)-JQ1 PA 1 Publications Verification		Alkynes
(+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal *(BET)* inhibitor JQ1, with an IC₅₀ of 10.4 nM. (+)-JQ1 PA 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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