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BRD4 BD-2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AMPK (1) Apoptosis (4) Bcl-2 Family (1) c-Myc (2) CDK (1) Epigenetic Reader Domain (62) Histone Acetyltransferase (1) HIV (1) Interleukin Related (1) Ligands for Target Protein for PROTAC (1) Molecular Glues (3) PAK (1) PI3K (1) PROTACs (13) TNF Receptor (1)
By Research Areas:	Cancer (50) Cardiovascular Disease (2) Infection (2) Inflammation/Immunology (16)
Click Chemistry:	PROTAC Synthesis (1)

Inhibitors & Agonists

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111433

BRD4 degrader AT1 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4* as a highly selective *Brd4* degrader, with a K_d of 44 nM for Brd4 ^BD2 in cells.

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-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-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-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-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) .

HY-142675

BRD4-BD1/2-IN-2	Epigenetic Reader Domain	Cancer
BRD4-BD1/2-IN-2 is a potent **BRD4 BD2 inhibitor with IC₅₀*s of <0.5 nM and <300 nM for BRD4* BD2 and BRD4 BD1, respectively (WO2021233371A1, compound 2) .

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) .

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-170380

XY221	Epigenetic Reader Domain Apoptosis AMPK c-Myc PAK Bcl-2 Family	Cancer
XY221 (Compound 16o) selectively inhibits **BRD4 BD2, with an IC₅₀** of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity .

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 .

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-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-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 .

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-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 .

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-143317

XY153	Epigenetic Reader Domain	Cancer
XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC₅₀s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .

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 .

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 .

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 . 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-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 .

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 .

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 .

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 .

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 .

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 .

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 .

HY-136571

GSK046 3 Publications Verification iBET-BD2	Epigenetic Reader Domain	Inflammation/Immunology
GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC₅₀s of 264 nM (BRD2 *BD2), 98 nM (BRD3* *BD2), 49 nM (BRD4* *BD2) and 214 nM (BRDT BD2*), respectively. GSK046 has immunomodulatory activity .

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 .

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-112376

MZP-54 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD3/4, with a K_d* of 4 nM for Brd4 ^BD2.

HY-112377

MZP-55 1 Publications Verification	Epigenetic Reader Domain PROTACs	Cancer
MZP-55 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD3/4, with a K_d* of 8 nM for Brd4 ^BD2.

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-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-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 .

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-114504

RVX-297	Epigenetic Reader Domain	Inflammation/Immunology
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for *BD2. RVX-297 shows IC₅₀s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2*), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models ^[2].

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-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-153241

GSK737	Epigenetic Reader Domain	Cancer
GSK737 is a BRD4 BD1 and *BD2* inhibitor, with pIC₅₀ values of 5.3 and 7.3 respectively. GSK737 has low clearance and good solubility and permeability in rat .

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-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-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-153894

SRX3177	CDK Epigenetic Reader Domain PI3K	Cancer
SRX3177 is a triple inhibitor of *CDK4/6, PI3K, and BRD4, with IC₅₀s of 33 nM (BRD4* BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ), <2.5 nM (CDK4), 3.3 nM (CDK6), respectively. SRX3177 exerts broad cytotoxic activity against cancer cells, but acts friendly with normal epithelial cells .

HY-153385

TMX1	Molecular Glues Epigenetic Reader Domain Apoptosis	Cancer
TMX1 is a *BRD4* covalent molecular glue degrader. TMX1 selectively recruits DCAF16 to the BRD4BD2, leading to BRD4 degradation.

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 .

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 . 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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