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Results for "

BET BD1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (3) Epigenetic Reader Domain (40) Histone Acetyltransferase (1) HIV (2) p38 MAPK (1) PROTACs (4)
By Research Areas:	Cancer (34) Infection (1) Inflammation/Immunology (12)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-162088

DW71177	Epigenetic Reader Domain	Inflammation/Immunology
DW71177 is a novel [1,2,4]triazolo[4,3-a] quinoxaline-based potent and BD1-Selective *BET* inhibitor, and can be used for study of acute myeloid leukemia .

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-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-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-102044

BET-IN-2

Epigenetic Reader Domain Cancer

BET-IN-2 is a BET inhibitor with an IC₅₀ of 52 nM for BRD4-BD1.

BET-IN-2	Epigenetic Reader Domain	Cancer
BET-IN-2 is a *BET* inhibitor with an IC₅₀ of 52 nM for BRD4-BD1.

HY-163271

XL-126	Epigenetic Reader Domain	Inflammation/Immunology
XL-126 (Compound 33) is a potent BD1-selective *BET* inhibitor, with a K_d of 8.9 nM. XL-126 leads to both the preservation of platelets and potent anti-inflammatory efficacy by BD1 selectivity .

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-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-149761

GSK023

Epigenetic Reader Domain Others

GSK023 (compound 31) is a selective chemical probe targeting the BET BD1 domain .
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-112609

QCA570

PROTACs Epigenetic Reader Domain Cancer

QCA570 is a PROTAC connected by ligands for Cereblon and BET, with an IC₅₀ of 10 nM for BRD4 BD1 Protein.

GSK023	Epigenetic Reader Domain	Others
GSK023 (compound 31) is a selective chemical probe targeting the BET BD1 domain .

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 .

QCA570	PROTACs Epigenetic Reader Domain	Cancer
QCA570 is a PROTAC connected by ligands for Cereblon and *BET, with an IC₅₀* of 10 nM for BRD4 BD1 Protein.

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-138623

GSK789	Epigenetic Reader Domain	Inflammation/Immunology Cancer
GSK789 is an effective, cell-permeable, and highly selective inhibitor of the BET family first bromodomain (BD1), with antitumor and immunomodulatory effects

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-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-146739

BRD4 Inhibitor-19	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-19 is a BET* inhibitor* with an IC₅₀ of 55 nM for BRD4-BD1. BRD4 Inhibitor-19 can be used for multiple myeloma research .

HY-12863

Pelabresib CPI-0610	Epigenetic Reader Domain	Cancer
Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active *BET* inhibitor. Pelabresib inhibits *BRD4-BD1* with an IC₅₀ of 39 nM, and with an EC₅₀ value of 0.18 μM for MYC .

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-146741

SDR-04	Epigenetic Reader Domain	Cancer
SDR-04 is a BET* inhibitor* and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation .

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-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-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-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-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-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-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-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-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-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-149735

BET-IN-20	Epigenetic Reader Domain Apoptosis	Cancer
BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC₅₀=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage .

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-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-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-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-136794

SB-284851-BT	p38 MAPK Epigenetic Reader Domain	Inflammation/Immunology Cancer
SB-284851-BT is an inhibitor of BRD4/p38α/BRDT. SB-284851-BT inhibits *BRD4-BD1* (IC₅₀=1.7 µM), p38α (K_d=0.47 nM), BRDT (1) (IC₅₀=18 µM) and BRD4 (1)(IC₅₀=3.7 µM). SB-284851-BT reduces IL-8 production by inhibiting p38α, as well as inhibiting BRD4 to down-regulates c-Myc and NF-κB gene pathways in cancer. SB-284851-BT can combined with the bromine domain and extra terminal (BET) .

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) .

HY-123911

dBET23

PROTACs Epigenetic Reader Domain Cancer

dBET23 is a highly effective and selective PROTAC BRD4 degrader with a DC_50/5h of ~ 50 nM for BRD4_BD1 protein .

dBET23	PROTACs Epigenetic Reader Domain	Cancer
dBET23 is a highly effective and selective PROTAC BRD4 degrader with a DC_50/5h of ~ 50 nM for BRD4_BD1 protein .

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BET BD1

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