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Results for "

BRD2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (4) E3 Ligase Ligand-Linker Conjugates (1) Epigenetic Reader Domain (38) Histone Acetyltransferase (1) HIV (1) Ligands for Target Protein for PROTAC (1) Molecular Glues (1) PROTACs (8) Small Interfering RNA (siRNA) (3)
By Research Areas:	Cancer (37) Infection (1) Inflammation/Immunology (7)

Inhibitors & Agonists

Antibodies

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-RS01597

BRD2 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
BRD2 Human Pre-designed siRNA Set A contains three designed siRNAs for BRD2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

BRD2 Human Pre-designed siRNA Set A BRD2 Human Pre-designed siRNA Set A

HY-RS01598

Brd2 Mouse Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Brd2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Brd2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Brd2 Mouse Pre-designed siRNA Set A Brd2 Mouse Pre-designed siRNA Set A

HY-RS01599

BRD2 Rat Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
BRD2 Rat Pre-designed siRNA Set A contains three designed siRNAs for BRD2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

BRD2 Rat Pre-designed siRNA Set A BRD2 Rat Pre-designed siRNA Set A

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. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .

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-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-13235

I-BET151 20+ 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 ^[2].

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 ^[2].

HY-121738

TC AC 28

Epigenetic Reader Domain Cancer

TC AC 28 is a high-affinity BET bromodomain ligand with K_d values of 40, 800 nM for Brd2(2), Brd2(1), respectively .

TC AC 28	Epigenetic Reader Domain	Cancer
TC AC 28 is a high-affinity BET bromodomain ligand with K_d values of 40, 800 nM for Brd2(2), Brd2(1), respectively .

HY-145264

OARV-771	Epigenetic Reader Domain PROTACs	Cancer
OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC₅₀s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively .

HY-130814

Thalidomide-NH-C4-NH2 TFA	E3 Ligase Ligand-Linker Conjugates	Cancer
Thalidomide-NH-C4-NH2 TFA (compound 29c) is an E3 ligase ligand-linker conjugate, and incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-NH-C4-NH2 TFA is used in PROTAC BRD2/BRD4 degrader-1 (HY-130612). PROTAC BRD2/BRD4 degrader-1 is a potent and selective BET protein BRD4 and BRD2 degrader .

HY-160528

IBG3	Epigenetic Reader Domain Molecular Glues	Cancer
IBG3 is a dual-JQ1-containing BET degrader that targets protein degradation via intramolecular bivalent glues. IBG3 is a *BRD2* and *BRD4* bifunctional degrader with DC₅₀ values of 8.6 pM and 6.7 pM, respectively .

HY-136571

GSK046 2 Publications Verification iBET-BD2	Epigenetic Reader Domain	Inflammation/Immunology
GSK046 (iBET-BD2) 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-100972

ARV-771 20+ Cited Publications	PROTACs Epigenetic Reader Domain	Cancer
ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with K_ds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for *BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2)*, respectively .

HY-15743

Birabresib Maximum Cited Publications 26 Publications Verification OTX-015; MK-8628	Epigenetic Reader Domain	Cancer
Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC₅₀s ranging from 92 to 112 nM.

HY-120000

MS402 1 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-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 .

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-107425

MZ 1 10+ Cited Publications	PROTACs Epigenetic Reader Domain	Cancer
MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2* and BRD3. K_ds of 382/120, 119/115, and 307/228 nM for **BRD4 BD1/2*, BRD3 BD1/2, and BRD2* BD1/2, respectively .

HY-103633

PROTAC BET Degrader-1 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.

HY-112429

HJB97 2 Publications Verification	Epigenetic Reader Domain	Cancer
HJB97 is a high-affinity BET inhibitor with K_is 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), 1.0 nM (BRD4 *BD2), respectively. HJB97 is employed for the design of potential PROTAC BET* degrader and has antitumor activity .

HY-19760

I-BET282
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-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-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-13960

GSK1324726A 5 Publications Verification I-BET726	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-15743A

(R)-Birabresib (R)-OTX-015; (R)-MK-8628	Others	Cancer
(R)-Birabresib is the isomer of Birabresib (HY-15743), and can be used as an experimental control. Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC₅₀s ranging from 92 to 112 nM.

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-19549

RX-37

RX-37 is a selective BET inhibitor. RX-37 binds to BET bromodomain proteins (BRD2, BRD3, and BRD4) with K_i values of 3.2-24.7 nM. RX-37 can be used for research of cancers .

RX-37
RX-37 is a selective BET inhibitor. RX-37 binds to BET bromodomain proteins (BRD2, BRD3, and BRD4) with K_i values of 3.2-24.7 nM. RX-37 can be used for research of cancers .

HY-126325

BY27	Epigenetic Reader Domain	Cancer
BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. Anti-cancer activity .

HY-141438

SIM1 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for *BRD2* degradation (IC₅₀=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity .

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-111422

PLX51107 3 Publications Verification	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-112090

ABBV-744 3 Publications Verification	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-151593

dBRD4-BD1	PROTACs Epigenetic Reader Domain	Cancer
dBRD4-BD1 is a selective and durable *BRD4* degrader with an DC₅₀ value of 280 nM (D_max=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1 .

HY-136570

GSK778 iBET-BD1	Epigenetic Reader Domain Apoptosis	Inflammation/Immunology Cancer
GSK778 (iBET-BD1) 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-134463

NHWD-870	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-142704

BRD4 D1-IN-1	Epigenetic Reader Domain	Cancer
BRD4 D1-IN-1 is a selective BRD4 D1 inhibitor (IC₅₀<0.092 µM). BRD4 D1-IN-1 has 18 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC .

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 BRD*4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models ^[2].

HY-142705

BRD4 D1-IN-2	Epigenetic Reader Domain	Cancer
BRD4 D1-IN-2 (compound 26) is a potent and selective BRD4 D1 inhibitor (IC₅₀<0.092 µM). BRD4 D1-IN-2 has 15 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC .

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-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-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-143317

XY153	Epigenetic Reader Domain	Cancer
XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC₅₀s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .

HY-129917

KB02-JQ1 2 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
KB02-JQ1 is a highly selective and PROTAC-based *BRD4* degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes *BRD4* degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1 .

HY-138563

GSK973	Epigenetic Reader Domain	Cancer
GSK973 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-153519

WWL0245	Epigenetic Reader Domain	Cancer
WWL0245 is a potent and seletive *BRD4* PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC₅₀ (<1 nM) than BRD2/3 and PLK1 ( DC₅₀>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 .

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