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BRD4(1) bromodomain

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) Autophagy (1) Drug Isomer (1) Drug Metabolite (1) Epigenetic Reader Domain (20) Histone Acetyltransferase (2) Ligands for Target Protein for PROTAC (1) Molecular Glues (1) Polo-like Kinase (PLK) (1)
By Research Areas:	Cancer (17) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (1)

Inhibitors & Agonists

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-15826

SGC-CBP30 15+ Cited Publications	Epigenetic Reader Domain Histone Acetyltransferase	Inflammation/Immunology Cancer
SGC-CBP30, a chemical probe, is a potent and highly selective CBP/p300 bromodomain (K_ds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of **BRD4 [BRD4(1)]** bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects .

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-120028

GNE-207	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
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-111976

MT1	Epigenetic Reader Domain	Cancer
MT1 is a bivalent chemical probe of BET bromodomains, with an IC₅₀ of 0.789 nM for BRD4(1) .

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-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-111502

Y06036	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-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 .

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 .

HY-117598

OXFBD03	Epigenetic Reader Domain	Others
OXFBD03 serves as an inhibitor of the BRD4(1) protein, which belongs to the bromodomain and extra terminal domain bromodomain family.

HY-103297

OXFBD02	Epigenetic Reader Domain	Cancer
OXF BD 02 is a selective inhibitor of *BRD4(1)* (the first bromodomain of BRD4) with IC₅₀ value of 382 nM .

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-111503

Y06137	Epigenetic Reader Domain	Cancer
Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the *BRD4(1)* bromodomain with a K_d of 81 nM .

HY-149806

Bromodomain IN-2	Epigenetic Reader Domain	Cancer
BD-IN-1 is a pan bromodomain (BD) inhibitor with K_D values of 250, 420, 130, 430, 67, 240, 970 nM for BRD4(1), CBP, BRPF1B, BRD7, BRD9, BRDT(1), CECR2 respectively. BD-IN-1 shows antiproliferative activity .

HY-150684

GXH-II-052	Epigenetic Reader Domain	Cancer
GXH-II-052 is a potent *bivalent bromodomain* and extraterminal domain (BET)** inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with K_d values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc .

HY-150683

NC-III-49-1	Epigenetic Reader Domain	Cancer
NC-III-49-1 is a potent *bivalent bromodomain* and extraterminal domain (BET)** inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with K_d values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc .

HY-155891

BET-IN-18	Epigenetic Reader Domain	Cancer
BET-IN-18 (Compound 3) is a pan-BET bromodomain small-molecule inhibitor, with K_i values of 0.69 μM and 0.37 μM, and K_d values of 1.6 μM and 8.4 μM against BrdT (1) and Brd4 (1) bromodomains, respectively. BET-IN-18 potently and competitively inhibits the binding of the known BET inhibitor (+)-JQ1 (HY-13030) to Brd4 (1) and BrdT (1), with IC₅₀ values of 1.0 μM and 2.3 μM, respectively. BET-IN-18 also competitively inhibits the binding of acetylated histone substrates to Brd4 (1) (IC₅₀ = 0.90 μM). BET-IN-18 can be used in the research of multiple myeloma .

HY-181976

dHTC3	Molecular Glues Epigenetic Reader Domain	Others
dHTC3 is a selective *BRD4* molecular glue degrader. dHTC3 specifically recruits the first bromodomain of BRD4 to the E3 ubiquitin ligase complex (SCF ^FBXO3), thereby triggering the ubiquitination and degradation of BRD4 .

HY-50698A

(S)-BI 2536	Drug Isomer Epigenetic Reader Domain Polo-like Kinase (PLK)	Cancer
(S)-BI 2536 (Compound 39g) is the enantiomer of BI 2536 (HY-50698). (S)-BI 2536 acts as an inhibitor of the *BRD4* bromodomain and PLK1 kinase, with a K_i value of 54 nM against BRD4 and a K_i value of 0.42 nM against PLK1 kinase. (S)-BI 2536 exhibits anticancer activity against acute myeloid leukemia. (S)-BI 2536 can be used for the research of acute myeloid leukemia .

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 .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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