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BRD2-BD1

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By Targets:	Apoptosis (2) c-Myc (1) E3 Ligase Ligand-Linker Conjugates (1) Epigenetic Reader Domain (15) Interleukin Related (1) Ligands for Target Protein for PROTAC (2) PROTACs (1) STAT (1)
By Research Areas:	Cancer (11) Inflammation/Immunology (7)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-162514

BBC0403	Epigenetic Reader Domain	Inflammation/Immunology
BBC0403 is a selective *BRD2* inhibitor with K_ds of 7.64 μM and 41.37 μM for BRD2 (BD2) and *BRD2 (BD1), respectively. BBC0403 exhibitS higher binding specificity for BRD2* compared to BRD3 and BRD4. BBC0403 has the potential for osteoarthritis (OA) research .

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-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-175678

*PROTAC BRD2 BD1* Degrader-1**	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD2 BD1 Degrader-1 (compound 21-1) is a potent and selective *BRD2 BD1* PROTAC degrader. PROTAC BRD2 BD1 Degrader-1 induces the association of BRD2 BD1 and von Hippel–Lindau-elongin C-elongin B (VCB). (Pink: BRD2-BD1 Ligand (HY-175679); Blue: E3 ligase ligand (HY-125845); Black: Linker (HY-W069332)) .

HY-175679

BRD2 BD1 ligand-1	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
BRD2 BD1 ligand-1 is a potent BRD2 BD1 ligand (Ligands for Target Protein for PROTACs) can be used in the synthesis of PROTAC BRD2 BD1 Degrader-1 (HY-175678) .

HY-175680

Boc-4-(3-oxobutyl)piperidine-(S,R,S)-AHPC	E3 Ligase Ligand-Linker Conjugates	Cancer
Boc-4-(3-oxobutyl)piperidine-(S,R,S)-AHPC is an E3 ligase ligand-linker conjugatecan be used in the synthesis of PROTAC BRD2 BD1 Degrader-1 (HY-175678) .

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-176535

KB-0118 BBC0115	Epigenetic Reader Domain Interleukin Related STAT	Inflammation/Immunology
KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with K_d values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model.

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-173062

BRD4 Inhibitor-40	Epigenetic Reader Domain c-Myc	Others
BRD4 Inhibitor-40 (Compound 23) is the inhibitor for BRD that inhibits BRD4-BD1, BRD4-BD2, *BRD2-BD1* and *BRD2-BD2* with IC₅₀s of 16.1, 142.18, 29.35 and 302.35 nM, respectively. BRD4 Inhibitor-40 modulates the expression of c-Myc and *p21*, arrests cell cycle at G1 phase, inhibits Pkd1-null (PN) renal cystic epithelial cells, and blocks the renal cysts formation in Madin-Darby canine kidney and embryonic kidney vesicle models. BRD4 Inhibitor-40 exhibits renal cysts inhibitory activity in mouse models .

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-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-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-183247

BRDT-IN-1	Epigenetic Reader Domain	Cancer
BRDT-IN-1 is a BRDT-BD1 and BRDT-T inhibitor with BRDT-BD1 IC₅₀ 19 nM, K_i 8.8 nM, K_a 1.6 nM, and BRDT-T IC₅₀ 56 nM, K_a 5.0 nM. BRDT-IN-1 displays in vitro metabolic stability and limited cellular permeability in MDCK-MDR1 cells. BRDT-IN-1 can be used for the research of multiple myeloma .

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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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BRD2-BD1

Inhibitors & Agonists