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Results for "

bromodomain+inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antibiotic (1) Apoptosis (10) ATP-binding cassette (ABC) transporters (1) Autophagy (1) Bacterial (1) c-Myc (1) CTLA-4 (1) Drug Intermediate (1) Drug Metabolite (1) Epigenetic Reader Domain (75) Fungal (1) Histone Acetyltransferase (7) HIV (1) HSP (1) Interleukin Related (1) LAG-3 (1) Ligands for Target Protein for PROTAC (4) MDM-2/p53 (2) Parasite (1) PD-1/PD-L1 (2) PROTACs (1) Reference Standards (6) STAT (1) SWI/SNF Complex (1)
By Research Areas:	Cancer (64) Cardiovascular Disease (2) Infection (3) Inflammation/Immunology (12) Metabolic Disease (2) Neurological Disease (2)

By Targets:

Antibiotic (1)

Apoptosis (10)

ATP-binding cassette (ABC) transporters (1)

Autophagy (1)

Bacterial (1)

c-Myc (1)

CTLA-4 (1)

Drug Intermediate (1)

Drug Metabolite (1)

Epigenetic Reader Domain (75)

Fungal (1)

Histone Acetyltransferase (7)

HIV (1)

HSP (1)

Interleukin Related (1)

LAG-3 (1)

Ligands for Target Protein for PROTAC (4)

MDM-2/p53 (2)

Parasite (1)

PD-1/PD-L1 (2)

PROTACs (1)

Reference Standards (6)

STAT (1)

SWI/SNF Complex (1)

By Research Areas:

Cancer (64)

Cardiovascular Disease (2)

Infection (3)

Inflammation/Immunology (12)

Metabolic Disease (2)

Neurological Disease (2)

Inhibitors & Agonists

Biochemical Assay Reagents

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13030

(+)-JQ-1 Maximum Cited Publications 295 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-13032

Molibresib 20+ 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-78695

JQ-1 carboxylic acid 5+ Cited Publications	Epigenetic Reader Domain PD-1/PD-L1 Ligands for Target Protein for PROTAC	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-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 1 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-12409

PFI-3 5 Publications Verification	Epigenetic Reader Domain	Cancer
PFI-3, a chemical probe, is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a K_d of 89 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-100482

CPI-637 10+ Cited Publications	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-136521

AZ13824374	Epigenetic Reader Domain	Cancer
AZ13824374 is a potent and selective ATAD2 bromodomain inhibitor (pIC₅₀ of 6.9 in HCT116 cells). AZ13824374 disrupts chromatin interactions and gene transcription by binding to the acetyl-lysine binding site of the ATAD2 bromodomain. AZ13824374 has anticancer activity against breast cancer .

HY-15658

GSK2801 3 Publications Verification	Epigenetic Reader Domain Apoptosis	Cancer
GSK2801, a chemical probe, is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with K_d values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4 .

HY-13959

MS436 1 Publications Verification	Epigenetic Reader Domain	Cancer
MS436 is a new class of *bromodomain* inhibitor, exhibits potent affinity of an estimated K_i=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2.

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-136571

GSK046 3 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-18665

GSK-5959	Epigenetic Reader Domain	Cancer
GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC₅₀ of ~ 80 nM .

HY-109050

Alobresib 2 Publications Verification GS-5829	Epigenetic Reader Domain	Cancer
Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research .

HY-100352

BI-9564 2 Publications Verification	Epigenetic Reader Domain	Cancer
BI-9564, a chemical probe, is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC₅₀s of 75 nM and 3.4 μM and K_ds of 14 nM and 239 nM, respectively. BI-9564 has an IC₅₀ of > 100 μM for BET family .

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-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-19336

BAZ2-ICR 2 Publications Verification	Epigenetic Reader Domain	Cancer
BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC₅₀s of 130 nM and 180 nM, and K_ds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe .

HY-151538

PBRM1-BD2-IN-8	Epigenetic Reader Domain	Cancer
PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 K_d=4.4 μM, PBRM1-BD2 IC₅₀=0.16 μM; PBRM1-BD5 K_d=25 μM). PBRM1-BD2-IN-8 shows anti-cancer activity .

HY-W010649

Isoxazole	HSP Epigenetic Reader Domain ATP-binding cassette (ABC) transporters Bacterial Fungal Antibiotic	Infection Metabolic Disease Inflammation/Immunology Cancer
Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor .

HY-111420

CBP/p300-IN-1	Epigenetic Reader Domain	Cancer
CBP/p300-IN-1 is a CBP/EP300 bromodomain inhibitor.

HY-114416

GS-626510	Epigenetic Reader Domain	Cancer
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-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-156744

DBr-1	PROTACs Epigenetic Reader Domain	Cancer
DBr-1 is a potent BRD9 PROTAC degrader (K_D: 13 nM). DBr-1 can overcome intrinsic resistance to VHL-degrader. Blue: DCAF1 binder (HY-149934), Black: linker, Pink: BRD9/BRD7 bromodomains inhibitor (HY-100352) .

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-151532

PBRM1-BD2-IN-5	Epigenetic Reader Domain	Cancer
PBRM1-BD2-IN-5 is a potent PBRM1 Bromodomain inhibitor with K_d values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC₅₀ value of 0.26 μM for PBRM1-BD2. PBRM1-BD2-IN-5 reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptide. PBRM1-BD2-IN-5 can be used to research anticancer .

HY-139148

UMB298	Epigenetic Reader Domain	Cancer
UMB298 is a potent and selective CBP/P300 bromodomain inhibitor .

HY-170817

SMI-1074	Ligands for Target Protein for PROTAC SWI/SNF Complex	Cancer
SMI-1074, a SMARCA bromodomain inhibitor, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). SMI-1074 can be used for synthesis SMD-3236 (HY-170824) and SMD-1087 (HY-170828). SMI-1074 can be used for the research of smarca4-deficient cancers .

HY-110315

Ischemin sodium	Apoptosis MDM-2/p53 Epigenetic Reader Domain	Cardiovascular Disease
Ischemin sodium is a CBP bromodomain inhibitor that inhibits p53 interaction with CBP and transcriptional activity in cells. Ischemin sodium salt inhibits p53-induced p21 activation with an IC₅₀ value of 5 µM. Ischemin sodium salt also prevents apoptosis in ischemic cardiomyocytes. Ischemin sodium salt can be used in the study of cardiovascular diseases (such as myocardial ischemia) .

HY-100697

TPOP146 3 Publications Verification	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with K_d values of 134 nM and 5.02 μM for CBP and BRD4.

HY-77826

4-Chloro-N-methylpicolinamide	Epigenetic Reader Domain	Cancer
4-Chloro-N-methylpicolinamide (Compound 3) is a BAZ2A bromodomain inhibitor with a K_d of >500 μM. 4-Chloro-N-methylpicolinamide forms a weak hydrogen bond with the carbonyl oxygen of Pro1817. 4-Chloro-N-methylpicolinamide can be used in the research of invasive prostate cancer .

HY-145431

(S)-GSK1379725A	Epigenetic Reader Domain Parasite	Infection
(S)-GSK1379725A (compound AU1) is a selective **bromodomain and PHD finger containing transcription factor (BPTF) bromodomain** inhibitor with a K_d of 2.8 μM. (S)-GSK1379725A shows to be selective for BPTF over BRD4 bromodomain. (S)-GSK1379725A shows antimalarial activity .

HY-151528

PBRM1-BD2-IN-1	Epigenetic Reader Domain	Cancer
PBRM1-BD2-IN-1 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-1 has binding affinity and inhibitory activity for PBRM1-BD2 with K_d and IC₅₀ values of 0.7 μM and 0.2 μM, respectively. PBRM1-BD2-IN-1 can be used for the research of cancer .

HY-151531

PBRM1-BD2-IN-4	Epigenetic Reader Domain	Cancer
PBRM1-BD2-IN-4 (compound 15) is a potent PBRM1 Bromodomain inhibitor with K_d values of 5.5 μM and 11.1 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC₅₀ value of 0.2 μM for PBRM1-BD2. PBRM1-BD2-IN-4 can be used to research anticancer .

HY-116349

Bromodomain IN-1	Epigenetic Reader Domain	Cancer
Bromodomain IN-1 is a *Bromodomain* inhibitor extracted from patent WO2016069578A1, compound 4 .

HY-78197

3,5-Dimethylisoxazole-4-boronic acid pinacol ester	Drug Intermediate	Others
3,5-Dimethylisoxazole-4-boronic acid pinacol ester is a drug intermediate that can be used for the synthesis of bromodomain inhibitors .

HY-128703

Bromodomain inhibitor-8	Epigenetic Reader Domain	Inflammation/Immunology
Bromodomain inhibitor-8 (example 1) is a BET bromodomain inhibitor for treating autoimmune and inflammatory diseases .

HY-153668

Bromodomain inhibitor-12	Epigenetic Reader Domain	Inflammation/Immunology
Bromodomain inhibitor-12 (example 303) is a *bromodomain* inhibitor that can be used in the research of autoimmune and inflammatory diseases .

HY-147375

Bromodomain inhibitor-10	Epigenetic Reader Domain	Cancer
Bromodomain inhibitor-10 (compound 128) is a potent *bromodomain* inhibitor with K_ds of 15.0, 2500 nM for BRD4-1 and BRD4-2, respectively. Bromodomain inhibitor-10 inhibits the production of IL12p40 .

HY-147374

Bromodomain inhibitor-9	Epigenetic Reader Domain	Metabolic Disease Inflammation/Immunology
Bromodomain inhibitor-9 is a *Bromodomains* inhibitor that selectively inhibits BRD4-1 (K_d: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases .

HY-153668A

Bromodomain inhibitor-12 (edisylate)	Epigenetic Reader Domain	Inflammation/Immunology
Bromodomain inhibitor-12 edisylate (example 303) is a *bromodomain* inhibitor that can be used in the research of autoimmune and inflammatory diseases .

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-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-122573

Bromodomain inhibitor-13	Epigenetic Reader Domain	Cancer
Bromodomain inhibitor-13 (Compound 1) is an analog of PFI-3 (HY-12409). Bromodomain inhibitor-13 is a bromodomain-containing protein (BCP) inhibitor. Bromodomain inhibitor-13 targets SMARCA2, SMARCA4, PB1(5), and second bromodomain of PB1 (PB1(2)) with K_D values of 37, 53, 30, and 190 nM, respectively .

HY-110315A

Ischemin	Epigenetic Reader Domain Apoptosis MDM-2/p53	Cardiovascular Disease
Ischemin is a CBP bromodomain inhibitor that inhibits p53 interaction with CBP and transcriptional activity in cells. Ischemin inhibits p53-induced p21 activation with an IC₅₀ value of 5 µM. Ischemin also prevents apoptosis in ischemic cardiomyocytes. Ischemin can be used in the study of cardiovascular diseases (such as myocardial ischemia) .

HY-161125

(+)-JQ1-OH	Drug Metabolite	Others
(+)-JQ1-OH is the major metabolite of (+)-JQ1(HY-13030). (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC_50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy .

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