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Results for "

BRD4-IN-1

" in MedChemExpress (MCE) Product Catalog:

標的別:	Akt (2) AMPK (1) Androgen Receptor (3) Apoptosis (17) Autophagy (2) Bcl-2 Family (1) c-Fms (1) c-Myc (6) Caspase (1) CDK (4) Discoidin Domain Receptor (1) DNA/RNA Synthesis (3) Drug Derivative (1) Drug Intermediate (1) E1/E2/E3 Enzyme (1) E3 Ligase Ligand-Linker Conjugates (3) Epigenetic Reader Domain (128) FLT3 (2) Fluorescent Dye (1) HDAC (2) Histone Acetyltransferase (5) HIV (1) HSP (2) Hsp-targeting Chimeras (1) Interleukin Related (3) JAK (3) Ligands for E3 Ligase (2) Ligands for Target Protein for PROTAC (4) Molecular Glues (5) NAMPT (1) Necroptosis (1) NF-κB (2) p38 MAPK (1) PAK (1) PARP (2) PI3K (4) Polo-like Kinase (PLK) (2) PROTAC Linkers (2) PROTACs (30) Reactive Oxygen Species (ROS) (1) Reference Standards (3) SARS-CoV (1) SNIPERs (1) STAT (1) Target Protein Ligand-Linker Conjugates (2) TNF Receptor (2)
研究分野別:	Cancer (122) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (22) Metabolic Disease (2) Neurological Disease (3)
クリックケミストリー:	PROTAC Synthesis (3) Azide (2) Alkynes (1)

140

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蛍光色素

天然物

クリックケミストリー

製品番号	製品名	Target	研究分野	構造式

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-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-176521

AR/BRD4 RIPTAC-1	Androgen Receptor Epigenetic Reader Domain	Cancer
AR/BRD4 RIPTAC-1 (Compound II-5) is an orally active Regulatory-inducible proximity-targeting chimera (RIPTAC). AR/BRD4 RIPTAC-1 induces the formation of a stable ternary complex between the androgen receptor (AR) and *BRD4, thereby blocking BRD4* function. AR/BRD4 RIPTAC-1 inhibits the growth and proliferation of tumor cells. AR/BRD4 RIPTAC-1 holds promise for use in prostate cancer research .

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-123844

dBET57 4 Publications Verification	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
dBET57 is an effective and selective *BRD4_BD1* degrader based on PROTAC technology, with the ability to induce cell apoptosis and anti-tumor activity. dBET57 mediates the recruitment of the E3 ubiquitin ligase CRL4 ^Cereblon, showing a DC_50/5h value of 500 nM for BRD4_BD1 .

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-100482

CPI-637 10+ Cited Publications	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-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-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-13959

MS436 1 Publications Verification	Epigenetic Reader Domain	Cancer
MS436 is a new class of bromodomain inhibitor, exhibits potent affinity of an estimated K_i=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2.

HY-145667

Biotinylated-JQ1 1 Publications Verification BiotIN-JQ1	Epigenetic Reader Domain	Cancer
Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for the bromodomain of *BRD4*. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC₅₀ of 0.4 μM .

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 .

HY-163638

*BRD4 degrader-1*	Epigenetic Reader Domain Molecular Glues E1/E2/E3 Enzyme	Cancer
BRD4 degrader-1 (Compound mL 1-50) is a relatively selective, monovalent and covalent *BRD4* Molecular glue degrader. BRD4 degrader-1 induces degradation of both long and short isoforms of *BRD4* by targeting DCAF16 (an E3 ligase). BRD4 degrader-1 can be used in breast cancer 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-156820

HLDA-221	Epigenetic Reader Domain	Cancer
HLDA-221 is a non-covalent regulated induced proximity targeting chimeras (RIPTAC). The binding of HLDA-221 to *BRD4-BD1* is significantly increased after pre-incubation with FKBP. HLDA-221 can be used in cancer research .

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-111976

MT1	Epigenetic Reader Domain	Cancer
MT1 is a bivalent chemical probe of BET bromodomains, with an IC₅₀ of 0.789 nM for BRD4(1) .

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* .

HY-114406

TD-106	Ligands for E3 Ligase	Cancer
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation .

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 .

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-111102

FL-411 BRD4-IN-1	Epigenetic Reader Domain	Cancer
FL-411 is a potent and selective *BRD4* inhibitor with an IC₅₀ of 0.43±0.09 μM for *BRD4(1)*.

HY-133138

Pomalidomide-PEG1-azide	E3 Ligase Ligand-Linker Conjugates	Cancer
Pomalidomide-PEG1-azide is an E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-PEG1-azide can be used to synthesis PROTAC BRD4 Degrader-1 (HY-133131) . 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.

HY-117491

BRD4 Inhibitor-10	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-10 (Compound II-25) is a potent *BRD4-BD1* inhibitor with an IC₅₀ of 8 nM. BRD4 Inhibitor-10 can be used to study diseases caused by abnormal or excessive cell proliferation, such as cancer .

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. ZL0590 can reduce mucosal inflammation in animal models of inflammatory bowel disease and restores tissue architecture. ZL0590 can be used in research on inflammatory diseases such as inflammatory bowel disease .

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-W017851

4-Phenyl-2-pyrrolidinone	Drug Intermediate	Neurological Disease
4-Phenyl-2-pyrrolidinone is a precursor and synthetic intermediate. 4-Phenyl-2-pyrrolidinone can be used as a precursor in the synthesis of compounds with anticonvulsant and nootropic activities and is an intermediate in the synthesis of bromodomain-containing protein 4 (BRD4) bromodomain 1 inhibitors .

HY-123621

GNE-375	Epigenetic Reader Domain	Cancer
GNE-375 is a potent and highly selective BRD9 inhibitor with an IC₅₀ of 5 nM. GNE-375 shows >100-fold selective for BRD9 over BRD4, TAF1, and CECR2. GNE-375 decreases BRD9 binding to chromatin .

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-156273

HDAC/JAK/BRD4-IN-1	Apoptosis HDAC Epigenetic Reader Domain JAK	Cancer
HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent *HDAC/JAK/BRD4* triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo .

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-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-123911

dBET23	PROTACs Epigenetic Reader Domain	Cancer
dBET23 is a highly effective and selective PROTAC *BRD4* degrader with a DC_50/5h of ~ 50 nM for BRD4_BD1 protein .

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-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-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-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-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-176369

*PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu*	Target Protein Ligand-Linker Conjugates Epigenetic Reader Domain	Cancer
PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for *BRD4* and a PROTAC linker. PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu can be used for synthesis of PROTAC BRD4 Degrader-14 (HY-138637) .

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-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-173450

ZL0516	Epigenetic Reader Domain	Inflammation/Immunology
ZL0516 is a potent, selective, and orally active *BRD4 BD1* inhibitor. ZL0516 suppresses inflammatory bowel disease (IBD) by inhibiting *BRD4/NF-κB* signaling .

HY-144338

PARP1/BRD4-IN-1	Epigenetic Reader Domain PARP Apoptosis DNA/RNA Synthesis	Cancer
PARP1/BRD4-IN-1 is a potent and high selective *PARP1/BRD4* inhibitor (IC₅₀s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells .

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-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-143471

WNY0824 PLK1/BRD4-IN-1	Polo-like Kinase (PLK) Epigenetic Reader Domain Apoptosis Androgen Receptor c-Myc	Cancer
WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC₅₀ values of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, *BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC*-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models .

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 .

製品番号	製品名		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.

HY-133138

Pomalidomide-PEG1-azide		Azide PROTAC Synthesis
Pomalidomide-PEG1-azide is an E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-PEG1-azide can be used to synthesis PROTAC BRD4 Degrader-1 (HY-133131) . 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.

HY-159777

JQ-1-PEG5-Alkyne		Alkynes
CPI-203-PEG5-Alkyne is a conjugate of target protein ligase and linker. CPI-203-PEG5-Alkyne can be used for synthesis of PROTAC BRD4-DCAF1 degrader-1 (HY-169151) .

HY-130984

Azido-PEG1-CH2COO-Cl		PROTAC Synthesis Azide
Azido-PEG1-CH2COO-Cl (compound 43a) is an alkyl/ether-based PROTAC linker. Azido-PEG1-CH2COO-Cl can be used in the synthesis of PROTAC BRD4 Degrader-1 (HY-133131) . Azido-PEG1-CH2COO-Cl is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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