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BRD4 BD-1 bromodomain

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By Targets:	Apoptosis (3) Epigenetic Reader Domain (34) Fluorescent Dye (1) Histone Acetyltransferase (3) Interleukin Related (1) Polo-like Kinase (PLK) (1) PROTACs (3) Reference Standards (1) STAT (1)
By Research Areas:	Cancer (28) Inflammation/Immunology (10)
Click Chemistry:	PROTAC Synthesis (1)

Inhibitors & Agonists

Fluorescent Dyes

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Products

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-136570

GSK778 1 Publications Verification iBET-BD1	Epigenetic Reader Domain Apoptosis	Inflammation/Immunology Cancer
GSK778 (iBET-BD1), a chemical probe, 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-114204

GSK8814 1 Publications Verification	Epigenetic Reader Domain	Cancer
GSK8814 is a potent and selective ATAD2 bromodomain chemical probe and inhibitor (IC₅₀ = 0.059 μM), with a binding constant pK_d = 8.1 and a pK_i = 8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with *pIC₅₀s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4* BD1. GSK8814 can be researched for cancer associated with ATAD2 bromodomain .**

HY-129937A

GNE-987 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
GNE-987 is a VHL-dependent BRD4 PROTAC degrader. 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 can be used for the research of cancer .

HY-100482

CPI-637 Maximum Cited Publications 13 Publications Verification	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC₅₀ values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and **BRD4 BD-1, respectively, and an EC₅₀ of 0.3 μM for CBP** .

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-151594

iBRD4-BD1	Epigenetic Reader Domain	Inflammation/Immunology Cancer
iBRD4-BD1 is selective **BRD4 bromodomain** inhibitor. iBRD4-BD1 has inhibition activity for BRD4 bromodomain with an IC₅₀ value of 12 nM. iBRD4-BD1 can be used for the research of inflammation and oncology .

HY-136857

BRD4 degrader-3	Epigenetic Reader Domain	Cancer
BRD4 degrader-3 is a potent **bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC₅₀*s of 15.5 and 12.3 nM for BRD4-BD1* and BRD4-BD2, respectively . PROTAC BRD4 Degrader-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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-125232

MS645 1 Publications Verification	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-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-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-124596

CD161	Epigenetic Reader Domain	Cancer
CD161 is a potent, selective and orally bioavailable **bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC₅₀*s of 28.2 nM and 7.2 nM for BRD4* BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity .

HY-112150

ZL0454 2 Publications Verification	Epigenetic Reader Domain	Inflammation/Immunology
ZL0454 is a potent and selective **Bromodomain-containing protein 4 (BRD4) inhibitor with an IC₅₀** of 49 and 32 nM for BD1 and BD2.

HY-146208

BRD4 Inhibitor-20 1 Publications Verification	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-20 is a potent orally active **bromodomain protein 4 (BRD4)** inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC₅₀ values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer .

HY-138563

GSK973	Epigenetic Reader Domain	Cancer
GSK973, a chemical probe, 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-112149

ZL0420	Epigenetic Reader Domain	Inflammation/Immunology
ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC₅₀ values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.

HY-160558

PLK1/BRD4-IN-3	Epigenetic Reader Domain Polo-like Kinase (PLK)	Cancer
PLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). PLK1/BRD4-IN-3 inhibits BRD4-BD1, PLK1 and BRDT-BD1, with IC₅₀s of 0.059, 0.127 and 0.245 μM, respectively .

HY-112149A

(E/Z)-ZL0420	Epigenetic Reader Domain	Inflammation/Immunology Cancer
(E/Z)-ZL0420 is a racemic compound of (Z)-ZL0420 and (E)-ZL0420 isomers. (E)-ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC₅₀ values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 .

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-N3213

Naringenin triacetate	Epigenetic Reader Domain	Cancer
Naringenin triacetate is a flavonoid isolated from plant, exhibits a good binding affinity with multiple crystal structures of first bromodomain BRD4 (BRD4 BD1) .

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-160557

PLK1/BRD4-IN-2	Epigenetic Reader Domain	Cancer
PLK1/BRD4-IN-2 (compound 15) is a BI-2536 (HY-50698) analog and dual inhibitor that targets both Polo-like kinase 1 (PLK1) and BRD4bromodomain (BRD4-BD1 IC₅₀=28 nM, PLK1 IC₅₀=40 nM) .

HY-176535

KB-0118 BBC0115	Epigenetic Reader Domain Interleukin Related STAT	Inflammation/Immunology
KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with K_d values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model.

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-151594A

iBRD4-BD1 diTFA	Epigenetic Reader Domain	Inflammation/Immunology Cancer
iBRD4-BD1 diTFA is selective **BRD4 bromodomain** inhibitor. iBRD4-BD1 diTFA has inhibition activity for BRD4 bromodomain with an IC₅₀ value of 12 nM. iBRD4-BD1 diTFA can be used for the research of inflammation and oncology .

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-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-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-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-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-W173361

CBP/p300-IN-24	Epigenetic Reader Domain	Others
CBP/p300-IN-24 is a selective CBP bromodomain inhibitor with an IC₅₀ of 32 μM, showing selectivity over *BRD4* BD-1 bromodomain. CBP/p300-IN-24 binds to the acetyl lysine binding pocket, forms hydrogen bonds with Asn1168 and a solvent-mediated hydrogen bond with Tyr1125, and forms hydrophobic interactions with Leu1120, Ile1122, and Val1174 .

HY-D3393

JQ1-FITC TFA	Fluorescent Dye Epigenetic Reader Domain	Cancer
JQ1-FITC TFA is a *BRD4*-binding fluorescent tracer. JQ1-FITC TFA binds to BRD4 BD1, BD2, recombinant bromodomains, and endogenous BRD4 in cell lysates. JQ1-FITC TFA can be used for the research of breast cancer and cancer (Ex/Em = 495/525 nm) .

HY-182577

CFT-743	PROTACs Epigenetic Reader Domain	Cancer
CFT-743, a PROTAC-based heterobifunctional degrader and BET inhibtor, is a degrader of BRD4 bromodomain 1 (BD1) with a DC₅₀ of 4.3 nM. CFT-743's antitumor activitiy is dependent on BET degradation and can be attenuated by Pomalidomide (HY-10984), which is a CRBN binding molecule. CFT-743 induces ubiquitination of BRD4 BD1. CFT-743 can be used for cancer research .

HY-100482R

CPI-637 (Standard)	Epigenetic Reader Domain Reference Standards Histone Acetyltransferase	Cancer
CPI-637 (Standard) is the analytical standard of CPI-637 (HY-100482). This product is intended for research and analytical applications. CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP .

JQ1-FITC TFA	Fluorescent Dyes
JQ1-FITC TFA is a *BRD4*-binding fluorescent tracer. JQ1-FITC TFA binds to BRD4 BD1, BD2, recombinant bromodomains, and endogenous BRD4 in cell lysates. JQ1-FITC TFA can be used for the research of breast cancer and cancer (Ex/Em = 495/525 nm) .

Naringenin triacetate	Flavonoids Classification of Application Fields Flavonones Rutaceae Plants Disease Research Fields Citrus Cancer Source Classification	Epigenetic Reader Domain
Naringenin triacetate is a flavonoid isolated from plant, exhibits a good binding affinity with multiple crystal structures of first bromodomain BRD4 (BRD4 BD1) .

Cat. No.	Product Name		Classification

HY-136857

BRD4 degrader-3		PROTAC Synthesis
BRD4 degrader-3 is a potent **bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC₅₀*s of 15.5 and 12.3 nM for BRD4-BD1* and BRD4-BD2, respectively . PROTAC BRD4 Degrader-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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BRD4 BD-1 bromodomain

Inhibitors & Agonists

Fluorescent Dyes

NaturalProducts

Click Chemistry

Natural
Products