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Results for "

BET BD2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Epigenetic Reader Domain (35) Histone Acetyltransferase (1) HIV (2) PROTACs (2)
By Research Areas:	Cancer (27) Infection (1) Inflammation/Immunology (11)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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-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-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-115867

GSK852

Epigenetic Reader Domain Cancer

GSK852 is a highly potent, second bromodomain (BD2)-selective, bromo and extra-terminal domain (BET) inhibitor (pIC₅₀ = 7.9).

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 .

GSK852	Epigenetic Reader Domain	Cancer
GSK852 is a highly potent, second bromodomain (BD2)-selective, bromo and extra-terminal domain (BET) inhibitor (pIC₅₀ = 7.9).

HY-132232

GSK097	Epigenetic Reader Domain	Cancer
GSK097 is a potent and selective Inhibitor of the second bromodomain (BD2) of the bromodomain and extra-terminal domain (BET) proteins. GSK097 displays 2000-fold selective for BD2 over BD1 (BRD4 data) with >1 mg/mL solubility in FaSSIF media .

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-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-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-137892

GSK620	Epigenetic Reader Domain	Inflammation/Immunology
GSK620 is a potent and orally active *pan-BD2* inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood .

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-115867A

(S)-GSK852

Epigenetic Reader Domain Cancer

(S)-GSK852 is a diastereomer of GSK852 (HY-115867). GSK852 is a BET inhibitor targeting BD2 (pIC₅₀=7.9) .

(S)-GSK852	Epigenetic Reader Domain	Cancer
(S)-GSK852 is a diastereomer of GSK852 (HY-115867). GSK852 is a BET inhibitor targeting *BD2* (pIC₅₀=7.9) .

HY-16652

Apabetalone Maximum Cited Publications 6 Publications Verification RVX-208; RVX000222	Epigenetic Reader Domain HIV	Cancer
Apabetalone (RVX-208) is an inhibitor of *BET* transcriptional regulators with selectivity for the second bromodomain. The IC₅₀s are 87 μM and 0.51 μM for BD1 and *BD2*, respectively .

HY-153242

GSK217	Epigenetic Reader Domain	Inflammation/Immunology
GSK217 is a potent, selective, and highly soluble bromo and extraterminal domain (BET) second bromodomain *(BD2)* inhibitor. GSK217 can be used for the research of oncology and immune inflammation research .

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-129201

ZEN-2759	Epigenetic Reader Domain	Cancer
ZEN-2759 is a potent *BET* (Bromodomain and Extra-Terminal Domain) inhibitor, with IC₅₀ values of 0.23, 0.08 and 0.28 μM for BRD4(BD1), *BRD4(BD2), and BRD4(BD1BD2)*, respectively .

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-111978

ZEN-3862	Epigenetic Reader Domain	Cancer
ZEN-3862 is a *BET* inhibitor with IC₅₀s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively. ZEN-3862 can be used to form PROTACs to induce degradation of BRD4 .

HY-125232

MS645	Epigenetic Reader Domain	Cancer
MS645 is a bivalent BET bromodomains (BrD) inhibitor with a K_i of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells .

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-111977

ZEN-3219	Epigenetic Reader Domain	Cancer
ZEN-3219 is a *BET* inhibitor with IC₅₀s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), *BRD4(BD2)* and *BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTAC*s to induce degradation of BRD4 .

HY-111979

ZEN-3411	Epigenetic Reader Domain	Cancer
ZEN-3411 is a *BET* inhibitor with IC₅₀s of 0.05, 0.05 and 0.06 μM for BRD4(BD1), *BRD4(BD2)* and *BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTAC*s to induce degradation of BRD4 .

HY-111139

MS417 3 Publications Verification GTPL7512	Epigenetic Reader Domain HIV	Infection Inflammation/Immunology
MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC₅₀s of 30, 46 nM and K_ds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC₅₀, 32.7 μM).

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-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-124596

CD161 NKR-P1A	Epigenetic Reader Domain	Cancer
CD161 (NKR-P1A) 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-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-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-130622

LT052	Epigenetic Reader Domain	Inflammation/Immunology
LT052 is a highly selective BET BD1 inhibitor with an IC₅₀ of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC₅₀=12.130 μM). LT052 has anti-inflammatory activity and can be used for acute gout arthritis research .

HY-129937

(S)-GNE-987	PROTACs Epigenetic Reader Domain	Cancer
(S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC₅₀=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC) .

HY-129937A

GNE-987	PROTACs Epigenetic Reader Domain	Cancer
GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC₅₀=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC₅₀=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC) .

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BET BD2

Inhibitors & Agonists