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Results for "

BET/BRD4 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (1) Apoptosis (13) Autophagy (2) c-Myc (1) Drug Metabolite (1) Epigenetic Reader Domain (79) HDAC (2) Histone Acetyltransferase (1) HIV (2) Ligands for Target Protein for PROTAC (7) p38 MAPK (1) PD-1/PD-L1 (1) Polo-like Kinase (PLK) (1) PROTACs (5) Reference Standards (1)
By Research Areas:	Cancer (73) Infection (2) Inflammation/Immunology (13)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-129939

PROTAC BRD4 ligand-1	Epigenetic Reader Domain Ligands for Target Protein for PROTAC	Cancer
PROTAC BRD4 ligand-1 is a potent *BET* inhibitor and a ligand for target *BRD4* protein for PROTACT GNE-987 (HY-129937A) .

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-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 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-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-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-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-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-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-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 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-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-150516S

BET-IN-12	Epigenetic Reader Domain	Cancer
BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC₅₀ of 0.9 nM for BRD4 .

HY-100653

AZD5153 1 Publications Verification	Epigenetic Reader Domain Apoptosis	Cancer
AZD5153 is a bivalent, selective, and orally active *BET/BRD4* bromodomain inhibitor with an IC₅₀ of value of 5 nM for full-length BRD4 (FL-BRD4). AZD5153 ligates two bromodomains in BRD4 simultaneously. AZD5153 can be used for the study of cancer, such as acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma .

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-111916

ODM-207 BET-IN-4	Epigenetic Reader Domain	Cancer
ODM-207 (BET-IN-4) is a potent *BET* bromodomain protein (BRD4) inhibitor, with an IC₅₀ of ≤ 1 μM .

HY-W806047

BRD4 Inhibitor-37	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-37 is a compound with anticancer activity that has inhibitory activity against BRD4. BRD4 Inhibitor-37 has an IC50 of approximately 0.05-0.1 μM in binding assays and shows a GI50 of 0.1-0.3 μM in cell-based assays. The effect of BRD4 Inhibitor-37 on c-Myc, a downstream protein of BRD4, has been validated, demonstrating its ability to intervene in this signaling pathway. BRD4 Inhibitor-37 exhibits selectivity among five different bromodomain proteins, enhancing its potential as a BET protein inhibitor .

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-114407

TD-428	PROTACs Epigenetic Reader Domain	Cancer
TD-428 is a PROTAC connected by ligands for Cereblon and *BRD4. TD-428 is a highly specific BRD4* degrader with a DC₅₀ of 0.32 nM . TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation .

HY-112316B

(Rac)-BAY1238097	Epigenetic Reader Domain	Cancer
(Rac)-BAY1238097 is a *BET* inhibitor, with an IC₅₀ of 1.02 μM for BRD4. Used in cancer research .

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-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-100653A

AZD5153 6-Hydroxy-2-naphthoic acid 1 Publications Verification	Epigenetic Reader Domain	Cancer
AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available *BET/BRD4* bromodomain inhibitor; disrupts BRD4 with an IC₅₀ of 1.7 nM.

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-16586

PFI-1 2 Publications Verification	Epigenetic Reader Domain Autophagy Apoptosis	Cancer
PFI-1 is a selective *BET* (bromodomain-containing protein) inhibitor for BRD4 with IC₅₀ of 0.22 μM in a cell-free assay.

HY-111502

Y06036	Epigenetic Reader Domain	Cancer
Y06036 is a potent and selective *BET* inhibitor, which binds to the *BRD4(1)* bromodomain with K_d value of 82 nM . Antitumor 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-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 .

HY-100015

Mivebresib 10+ Cited Publications ABBV-075	Epigenetic Reader Domain Apoptosis	Cancer
Mivebresib (ABBV-075) is a potent and orally active *bromodomain and extraterminal domain (BET) bromodomain* inhibitor. Mivebresib binds to *BRD4* with a K_i of 1.5 nM .

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 .

HY-13235

I-BET151 25+ 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 .

HY-15846

CPI-203 4 Publications Verification	Epigenetic Reader Domain Apoptosis	Cancer
CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC₅₀ value of appr 37 nM (BRD4 α-screen assay).

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-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-107443

I-BET762 carboxylic acid Molibresib carboxylic acid; GSK525762A carboxylic acid; PROTAC BRD4-binding moiety 2	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a *BRD4* inhibitor with a pIC₅₀ of 5.1 .

HY-111503

Y06137	Epigenetic Reader Domain	Cancer
Y06137 is a potent and selective *BET* inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the *BRD4(1)* bromodomain with a K_d of 81 nM .

HY-150684

GXH-II-052	Epigenetic Reader Domain	Cancer
GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with K_d values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc .

HY-100696

PNZ5	Epigenetic Reader Domain	Cancer
PNZ5 is a potent and isoxazole-based *pan-BET* inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a K_D of 5.43 nM for BRD4(1) .

HY-150683

NC-III-49-1	Epigenetic Reader Domain	Cancer
NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with K_d values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc .

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-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-19549

RX-37	Epigenetic Reader Domain	Cancer
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-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-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-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-107443A

(R)-I-BET762 carboxylic acid (R)-Molibresib carboxylic acid; (R)-GSK525762A carboxylic acid; (R)-PROTAC BRD4-binding moiety 2	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
(R)-I-BET762 carboxylic acid, the R-enantiomer of I-BET762 carboxylic acid (HY-107443). I-BET762 carboxylic acid is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid is a *BRD4* inhibitor with a pIC₅₀ value of 5.1 .

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-135236

OXFBD04	Epigenetic Reader Domain	Cancer
OXFBD04 is a potent and selective *BRD4* inhibitor with an IC₅₀ of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity .

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-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 .

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