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BRD4 BD-2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) AMPK (1) Apoptosis (5) Bcl-2 Family (1) c-Fms (1) c-Myc (4) CDK (3) Discoidin Domain Receptor (1) DNA/RNA Synthesis (1) Epigenetic Reader Domain (75) Fluorescent Dye (1) Histone Acetyltransferase (1) HIV (1) Interleukin Related (2) Ligands for Target Protein for PROTAC (1) Molecular Glues (3) NF-κB (2) PAK (1) Phosphatase (1) PI3K (3) PROTACs (17) Reactive Oxygen Species (ROS) (1) SARS-CoV (1) TNF Receptor (2)
By Research Areas:	Cancer (61) Cardiovascular Disease (2) Endocrinology (1) Infection (3) Inflammation/Immunology (20) Metabolic Disease (1) Neurological Disease (1)
Click Chemistry:	PROTAC Synthesis (1)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-16954

ARV-825 Maximum Cited Publications 35 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-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-111433

BRD4 degrader AT1 2 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-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-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-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-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 ^[2] ^[4] .

HY-136571

GSK046 3 Publications Verification iBET-BD2	Epigenetic Reader Domain	Inflammation/Immunology
GSK046 (iBET-BD2), a chemical probe, 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-162514

BBC0403	Epigenetic Reader Domain	Inflammation/Immunology
BBC0403 is a selective *BRD2* inhibitor with K_ds of 7.64 μM and 41.37 μM for **BRD2 (BD2)** and BRD2 (BD1), respectively. BBC0403 exhibitS higher binding specificity for BRD2 compared to BRD3 and BRD4. BBC0403 has the potential for osteoarthritis (OA) research .

HY-120000

MS402 2 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-112376

MZP-54 2 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-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-156828

MMH2	Molecular Glues Epigenetic Reader Domain	Cancer
MMH2 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4_BD2) .

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-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-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-156827

MMH1	Molecular Glues Epigenetic Reader Domain	Cancer
MMH1 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4_BD2) .

HY-153385

TMX1	Molecular Glues Epigenetic Reader Domain	Cancer
TMX1 is a covalent, selective *BRD4* molecular glue degrader. TMX1 binds to the JQ1-binding site of *BRD4BD2, forms covalent bonds with Cys58 of DCAF16* and Cys87 of GAK in a *BRD4BD2*-dependent template-assisted manner, stabilizes the *BRD4-TMX1-DCAF16* ternary complex, and promotes the ubiquitination of *BRD4* via the CRL4_DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of *BRD4, mild degradation of BRD2* and BRD3, as well as DCAF16-dependent cytotoxicity ^[2].

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-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-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-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-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-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-163729

I-BET787	Epigenetic Reader Domain	Inflammation/Immunology Cancer
I-BET787 is a orally active BET bromine domain inhibitor with pIC₅₀s of 7.1 and 5.9 for BRD4 BD1 and BRD4 BD2, respectively. I-BET787 has anti-inflammatory activity in mice .

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-130622

LT052 1 Publications Verification	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-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-153894

SRX3177	CDK Epigenetic Reader Domain PI3K NF-κB SARS-CoV	Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
SRX3177 is a triple inhibitor of *CDK4/6, PI3K, and BRD4, with IC₅₀s of <2.5 nM (CDK4), 3.3 nM (CDK6), 33 nM (BRD4* BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ) , respectively. SRX3177 blocks the interaction between the SARS-CoV-2 E protein and the *BRD2/4* BD1 domain, restores E protein-attenuated NF-κB activity. SRX3177 exerts broad cytotoxic activity against cancer cells. SRX3177 can be used for the study of anti-SARS-CoV-2 and cancer ^[2].

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-178041

BRD4-BD1/2-IN-3	Epigenetic Reader Domain Interleukin Related c-Fms NF-κB TNF Receptor	Inflammation/Immunology
BRD4-BD1/2-IN-3 (Compound B6) is a selective **BRD4 BD2 inhibitor with an IC₅₀** of 0.41  nM for BRD4 BD2 over BRD4 BD1. BRD4-BD1/2-IN-3 significantly inhibits the LPS (HY-D1056)-induced expression of IL-6. BRD4-BD1/2-IN-3 shows anti-inflammatory activities by modulating the TNF and NF-κB signaling pathway. BRD4-BD1/2-IN-3 can be used for inflammatory diseases research .

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-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-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-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-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-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-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-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-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-174920

PROTAC BRD4 Degrader-34	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-34 (Compound MZ2) is a selective BRD4 PROTAC degrader (pDC₅₀ = 8.4). PROTAC BRD4 Degrader-34 can induce BD2 degradation mediated by VHL. PROTAC BRD4 Degrader-34 can be used for research on cancer. (Pink: BRD4-BD2 Ligand (HY-78695); Blue: VHL Ligand (HY-125845); Black: Linker (HY-130524)) .

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-176035

MS479	PROTACs Epigenetic Reader Domain	Cancer
MS479 is a BRD4 PROTAC degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: K_d = 200 nM; GLP: K_d = 306 nM). MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells. (Pink: BRD4 ligand (HY-78695); Blue: GLP ligand (HY-176036); Black: linker (HY-176037); GLP ligand+linker: HY-176038) .

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-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-178510

JQ1-S(GlcNAc)Cq	PROTACs Epigenetic Reader Domain	Cancer
JQ1-S(GlcNAc)Cq is a sugar-coated *BRD4* PROTAC degrader. JQ1-S(GlcNAc)Cq can inhibit the formation of the ternary complex between CRBN and BRD4(BD1/BD2). JQ1-S(GlcNAc)Cq can be used for the research of cancer . (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: CRBN ligand (HY-178514); Black: linker (HY-W105727); BRD4 ligand-Linker: (HY-178519))

HY-175033

BRD4-IN-11	Epigenetic Reader Domain Phosphatase c-Myc Apoptosis	Inflammation/Immunology
BRD4-IN-11 is an orally active and selective *BRD4* inhibitor (IC₅₀ = 26.35 nM (BD1), IC₅₀ = 72.81 nM (BD2)). BRD4-IN-11 is approximately 3- to 18-fold more potent against *BRD4* than againstBRD2, *BRD3, and BRDT. BRD4-IN-11* enhances H2S release and inhibits the upregulation of fibrotic markers (α-SMA and fibronectin), c-Myc, and CDC25B. BRD4-IN-11 reduces apoptosis in LO2 hepatocytes. BRD4-IN-11 significantly improves liver and lung function in a hepatopulmonary fibrosis model and can be used to study hepatopulmonary fibrosis .

HY-169355

TrimTAC1	PROTACs Epigenetic Reader Domain	Cancer
TrimTAC1 is a TRIM21-based PROTAC targeting BRD4. TrimTAC1 selectively degrads NUP98 ^FG-mEGFP-BRD4 ^BD2 nuclear condensates. TrimTAC1 does not degrade soluble mEGFP-BRD4 ^BD2 in A549 cells. (Pink: target protein ligand (+)-JQ-1 (HY-13030); Blue:E3 ligase ligand Acepromazine-OTs (HY-169356); Black: PROTAC linker (HY-W088456); E3 ligase ligand + linker: HY-169357) .

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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BRD4 BD-2

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