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Results for "

BET BD1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (4) Epigenetic Reader Domain (48) Histone Acetyltransferase (1) HIV (2) Ligands for Target Protein for PROTAC (1) p38 MAPK (1) PI3K (1) PROTACs (4)
By Research Areas:	Cancer (39) Infection (1) Inflammation/Immunology (15)

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	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-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-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-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-102044

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

HY-172210

DDO-8958	Epigenetic Reader Domain Apoptosis	Cancer
DDO-8958 is an orally active and selective **BET BD1 inhibitor with a K_D** of 5.6 nM for BRD4 BD1. DDO-8958 exhibits low nanomolar inhibitory activity against all **BET BD1** bromodomains except for BRDT BD1. DDO-8958 can inhibit the proliferation and migration, induce apoptosis and cell cycle arrest of tumor cells. DDO-8958 has anti-tumor activity .

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-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.

HY-162622

BET-IN-26	Epigenetic Reader Domain	Inflammation/Immunology
BET-IN-26 (compound 13a) is a potent, selective and orally active *BD1* inhibitor with IC₅₀ values of 0.0055, 9.0 µM for BD1, BD2, respectively. BET-IN-26 decreases LPS (HY-D1056) induced serum levels of IL-6 and MCP-1 .

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-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-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-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-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-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-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-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-162621

BET-IN-25	Epigenetic Reader Domain	Inflammation/Immunology
BET-IN-25 (compound 7) is an oral bioactive inhibitor of bromodomain (BD1) and BD2, with the IC₅₀s of 0.18 μM and 9.2 μM, respectively .

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-170226

BET-IN-28	Epigenetic Reader Domain	Cancer
BET-IN-28 (Compound 44) is a highly potent inhibitor of bromodomain and extra-terminal domain (BET), with an IC₅₀ value of 4.47 nM against BRD4-BD1. BET-IN-28 blocks the interaction between BET proteins and N-acetylated lysine residues on histone tails, down-regulates certain genes. BET-IN-28 can be used for hematological malignancies and solid tumors study .

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-172130

PI3Kδ/BET-IN-1	PI3K Epigenetic Reader Domain	Cancer
PI3Kδ/BET-IN-1 (compound 10b) shows excellent and balanced activities against PI3Kδ (IC₅₀ = 112 nM) and BRD4-BD1 (IC₅₀ = 19 nM) and exhibits strong antiproliferative activities in DLBCL cells .

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-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-111139

MS417 4 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-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-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-124596

CD161	Epigenetic Reader Domain	Cancer
CD161 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-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-145550

Amredobresib BI894999	Epigenetic Reader Domain	Cancer
Amredobresib (BI894999) is an orally active *BET* inhibitor. Amredobresib inhibits the binding of *BRD4-BD1* and BRD4-BD2 bromodomains to acetylated histones with IC₅₀ values of 5 nM and 41 nM, respectively. Amredobresib exhibits anticancer activity against acute myeloid leukemia (AML) and NUT cancer .

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-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 1 Publications Verification	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 .

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BET BD1

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