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BRD4 BD-1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AMPK (1) Apoptosis (9) Bcl-2 Family (1) c-Myc (3) Caspase (1) CDK (1) Epigenetic Reader Domain (84) Histone Acetyltransferase (2) HIV (2) Interleukin Related (1) Ligands for Target Protein for PROTAC (1) p38 MAPK (1) PAK (1) PI3K (2) Polo-like Kinase (PLK) (1) PROTACs (18) TNF Receptor (1)
By Research Areas:	Cancer (72) Cardiovascular Disease (2) Infection (3) Inflammation/Immunology (21)
Click Chemistry:	PROTAC Synthesis (1)

Inhibitors & Agonists

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Products

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-145310

ZL0590	Epigenetic Reader Domain	Inflammation/Immunology
ZL0590 is a potent, orally active **BRD4 BD1**-selective inhibitor with an IC₅₀ of 90 nM for human BRD4 BD1. ZL0590 exhibits significant anti-inflammatory activities ^[1].

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 ^[1].

HY-163413

BRD4-BD1-IN-3	Epigenetic Reader Domain	Inflammation/Immunology
BRD4-BD1-IN-3 (Compound 4g) is a *BRD4-BD1* inhibitor. BRD4-BD1-IN-3 can be used for research of inflammatory disease ^[1].

HY-143299

BRD4-BD1-IN-1	Epigenetic Reader Domain	Cancer
BRD4-BD1-IN-1 (Compound 9a) is a *BRD4-BD1* inhibitor with an IC₅₀ of 38.20 μM ^[1].

HY-143300

BRD4-BD1-IN-2	Epigenetic Reader Domain	Cardiovascular Disease Cancer
BRD4-BD1-IN-2 is a selective *BRD4-BD1* inhibitor, with an IC₅₀ of 2.51 µM (20-times greater than that of BD2). BRD4-BD1-IN-2 can be used in studies of cancer and cardiovascular diseases ^[1].

HY-142674

BRD4-BD1/2-IN-1	Epigenetic Reader Domain	Cancer
BRD4-BD1/2-IN-1 is a potent *BRD4* inhibitor with IC₅₀s of <100 nM for BRD4 BD-1 and BRD4 BD-2, respectively (US20150148375A1, compound 5) ^[1].

HY-142675

BRD4-BD1/2-IN-2	Epigenetic Reader Domain	Cancer
BRD4-BD1/2-IN-2 is a potent BRD4 BD2 inhibitor with IC₅₀s of <0.5 nM and <300 nM for BRD4 BD2 and BRD4 BD1, respectively (WO2021233371A1, compound 2) ^[1].

HY-147573

BRD4 Inhibitor-23	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-23 is a potent and orally active *BRD4* inhibitor with IC₅₀s of 6.21 nM and 1.44 nM for BRD4 BD-1 and BRD4 BD-2, respectively (WO2022033542A1; Example 1) ^[1].

HY-149519

BRD4 Inhibitor-28	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-28 (Compound 18) is an orally active *BRD4* Inhibitor. BRD4 Inhibitor-28 inhibits BRD40-BD1, BRD40-BD2 with IC₅₀s of 15, 55 nM. BRD4 Inhibitor-28 also inhibits BRD2-BD1, BRD3-BD1, BRDT-BD1 with IC₅₀s of 19, 25, 68 nM. BRD4 Inhibitor-28 has anti-melanoma activity ^[1].

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 ^[1].

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 ^[1].

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-133136

PROTAC BRD4 Degrader-2	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and *BRD4* with an IC₅₀ of 14.2 nM against **BRD4 BD1** ^[1].

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* ^[1].

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* ^[1].

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 ^[1].

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 ^[1].

HY-117491

BRD4 Inhibitor-10	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-10 is a potent *BRD4-BD1* inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC₅₀ of 8 nM ^[1].

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-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 ^[1].

HY-107425

MZ 1 15+ Cited Publications	PROTACs Epigenetic Reader Domain	Cancer
MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4* over BRD2 and BRD3. K_ds of 382/120, 119/115, and 307/228 nM for **BRD4 BD1/2*, BRD3 BD1/2, and BRD2 BD1*/2, respectively ^[1].

HY-155078

BRD4 Inhibitor-27	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-27 (compound 6) is a *BRD4* inhibitor with IC₅₀ of 9.6 and 11.3 μM for **BRD4 BD1** and BRD4 BD2, respectively. BRD4 Inhibitor-27 has the potential to study cancer ^[1].

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 ^[1].

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 ^[1].

HY-133131

PROTAC BRD4 Degrader-1	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and *BRD4* with an IC₅₀ of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression ^[1].

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-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 ^[1].

HY-160634

BRD4 Inhibitor-31	Epigenetic Reader Domain	Infection Inflammation/Immunology Cancer
BRD4 Inhibitor-31 (Example 136) is a *BRD4* inhibitor (K_is: 0.234 μM and 0.295 μM for BRD4 BD1 and BRD4 BD2 respectively). BRD4 Inhibitor-31 can be used for research of inflammatory diseases, cancer, and AIDS ^[1].

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) ^[1].

HY-16954

ARV-825 Maximum Cited Publications 21 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
ARV-825 is a PROTAC connected by ligands for Cereblon and *BRD4. ARV-825 binds to BD1* and BD2 of BRD4 with K_ds of 90 and 28 nM, respectively.

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 ^[1].

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 ^[1].

HY-152209

BRD4 Inhibitor-26	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-26 is a bromodomain protein 4 (BRD4) inhibitor/nitric oxide-donator. BRD4 Inhibitor-26 inhibits BRD4 (BD1) and BRD4 (BD2) with IC₅₀ values of 0.82 μM and 1.94 μM, respectively. BRD4 Inhibitor-26 can be used for the research of ovarian cancer ^[1].

HY-173062

BRD4 Inhibitor-40	Epigenetic Reader Domain c-Myc	Others
BRD4 Inhibitor-40 (Compound 23) is the inhibitor for *BRD* that inhibits *BRD4-BD1, BRD4-BD2, BRD2-BD1* and *BRD2-BD2* with IC₅₀s of 16.1, 142.18, 29.35 and 302.35 nM, respectively. BRD4 Inhibitor-40 modulates the expression of c-Myc and p21, arrests cell cycle at G1 phase, inhibits Pkd1-null (PN) renal cystic epithelial cells, and blocks the renal cysts formation in Madin-Darby canine kidney and embryonic kidney vesicle models. BRD4 Inhibitor-40 exhibits renal cysts inhibitory activity in mouse models ^[1].

HY-138555

PROTAC BRD4 Degrader-8	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4, with IC₅₀s of 1.1 nM and 1.4 nM for *BRD4 BD1 and BD2*, respectively. PROTAC BRD4* Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells ^[1].

HY-138637

PROTAC BRD4 Degrader-14	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-14 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4, with IC₅₀s of 1.8 nM and 1.7 nM for *BRD4 BD1 and BD2*, respectively. PROTAC BRD4* Degrader-14 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells ^[1].

HY-139294

PROTAC BRD4 Degrader-15	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-15 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4, with IC₅₀s of 7.2 nM and 8.1 nM for *BRD4 BD1 and BD2*, respectively. PROTAC BRD4* Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells ^[1].

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 IC₅₀s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively ^[1]. 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-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-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 ^[1].

HY-W265951

3-Methylcarbostyril	Epigenetic Reader Domain	Cancer
3-Methylcarbostyril (compound 5) is a **BRD4 BD1 inhibitor with a pIC₅₀** of 4.4 ^[1].

HY-170686

BRD4 Inhibitor-38	Interleukin Related TNF Receptor Epigenetic Reader Domain	Inflammation/Immunology
BRD4 Inhibitor-38 (Compound 25) is an orally active inhibitor of *BRD4* with IC₅₀ values of 3.64 μM and 0.12 μM against **BRD4 BD1** and BRD4 BD2, respectively. BRD4 Inhibitor-38 also exhibits anti-inflammatory activity, with an IC₅₀ value of 1.98 μM for inhibiting nitric oxide (NO) production ^[1].

HY-151972

BRD4 Inhibitor-25	Epigenetic Reader Domain	Cardiovascular Disease Inflammation/Immunology Cancer
BRD4 Inhibitor-25 is a *BRD4* inhibitor with IC₅₀s of 0.82 μM, 1.94 μM for BD1 and BD2 domains of BRD4. BRD4 Inhibitor-25 induces apoptotic and autophagy cell death in ovarian cancer cells. BRD4 Inhibitor-25 can be used in the research of cancers, cardiovascular, neuromuscular and inflammatory disorders.

HY-146208

BRD4 Inhibitor-20	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 ^[1].

HY-143327

PROTAC BRD4 Degrader-16	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
PROTAC BRD4 Degrader-16 is a potent PROTAC BRD4 Degrader, with IC₅₀ values of 34.58 nM (BRD4 *(BD1)) and 40.23 nM (BRD4* (BD2)). PROTAC BRD4 Degrader-16 ignificantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-16 significantly induces apoptosis in MV-4-11 cells ^[1].

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) ^[1].

HY-143328

PROTAC BRD4 Degrader-17	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC₅₀ values of 29.54 nM (BRD4 *(BD1)) and 3.82 nM (BRD4* (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells ^[1].

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 ^[1].

HY-112150

ZL0454	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-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 ^[1].

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 IC₅₀s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively ^[1]. 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

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