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BRD4-IN-1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (1) Apoptosis (12) Autophagy (1) c-Myc (2) Caspase (1) CDK (1) DNA/RNA Synthesis (2) E3 Ligase Ligand-Linker Conjugates (3) Epigenetic Reader Domain (87) HDAC (1) Histone Acetyltransferase (2) HIV (1) JAK (1) Ligands for E3 Ligase (2) Ligands for Target Protein for PROTAC (3) Molecular Glues (1) NAMPT (1) p38 MAPK (1) PARP (2) PI3K (1) Polo-like Kinase (PLK) (2) PROTAC Linkers (2) PROTACs (18)
By Research Areas:	Cancer (85) Cardiovascular Disease (1) Infection (2) Inflammation/Immunology (14) Neurological Disease (1)
Click Chemistry:	PROTAC Synthesis (2) Azide (3) Alkynes (1)

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Targets Recommended: AIM2 NEKs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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 .

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 .

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-169151

*PROTAC BRD4-DCAF1* degrader-1**	PROTACs Epigenetic Reader Domain Ligands for E3 Ligase	Cancer
PROTAC BRD4-DCAF1 degrader-1 (I-907) is a *BRD4-DCAF1* PROTAC degrader, DC₅₀ is 10~100 nM. (Pink: BRD4-DCAF1 ligand (HY-169152); Black: linker (HY-126976); Blue: E3 ligase ligand (HY-15846)) .

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-142704

BRD4 D1-IN-1	Epigenetic Reader Domain	Cancer
BRD4 D1-IN-1 is a selective *BRD4 D1* inhibitor (IC₅₀<0.092 µM). BRD4 D1-IN-1 has 18 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC .

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-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-142705

BRD4 D1-IN-2	Epigenetic Reader Domain	Cancer
BRD4 D1-IN-2 (compound 26) is a potent and selective *BRD4 D1* inhibitor (IC₅₀<0.092 µM). BRD4 D1-IN-2 has 15 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC .

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 .

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 .

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-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-146741

SDR-04	Epigenetic Reader Domain	Cancer
SDR-04 is a BET inhibitor and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation .

HY-169152

DCAF1 ligand 1	Ligands for Target Protein for PROTAC	Others
DCAF1 ligand 1 (compound I-653) is the ligand for target protein for PROTAC BRD4-DCAF1 degrader-1 (HY-169151) which has a DC₅₀ of 10~100 nM .

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-163638

*BRD4 degrader-1*	Molecular Glues Epigenetic Reader Domain	Cancer
BRD4 degrader-1 (Compound ML 1-50) is a monovalent and covalent molecular glue *BRD4* degrader. BRD4 degrader-1 targets DCAF16 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells .

HY-161515

BRD4/NAMPT-IN-1	NAMPT Epigenetic Reader Domain	Cancer
BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and *BRD4* (IC₅₀=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects .

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) .

HY-160672

BRD4-IN-8	Epigenetic Reader Domain	Cancer
BRD4-IN-8 (Example 13b) is a *BRD4* inhibitor .

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-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-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-159777

CPI-203-PEG5-Alkyne	E3 Ligase Ligand-Linker Conjugates	Cancer
CPI-203-PEG5-Alkyne is a conjugate of E3 ligase and linker. CPI-203-PEG5-Alkyne can be used for synthesis of PROTAC BRD4-DCAF1 degrader-1 (HY-169151) .

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-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-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-W265951

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

HY-123844

dBET57 2 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-145226

XY-06-007	PROTACs Epigenetic Reader Domain	Cancer
XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4_BD1L94V degrader. XY-06-007 shows a DC_{50, 6 h} of 10 nM against BRD4_BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies .

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-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-100670

Olinone	Epigenetic Reader Domain	Neurological Disease
Olinone is a selective *BRD4 BrD1* inhibitor . Olinone accelerates the progression of mouse primary oligodendrocyte progenitors toward differentiation .

HY-110378

ISOX-DUAL	Epigenetic Reader Domain	Others
ISOX-DUAL is a dual *CBP/BRD4* inhibitor with IC₅₀ values of 0.65 μM and 1.5 μM for CBP and BRD4, respectively .

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-114204

GSK8814	Epigenetic Reader Domain	Cancer
GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, 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 .

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-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-129939

PROTAC BRD4 ligand-1	Epigenetic Reader Domain Ligands for Target Protein for PROTAC	Cancer
PROTAC BRD4 ligand-1 is a potent BET inhibitor and a ligand for target *BRD4* protein for PROTACT GNE-987 (HY-129937A) .

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-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-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-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.

Cat. No.	Product Name		Classification

HY-133138

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

HY-108369

Azido-PEG1-CH2CO2H		Azide PROTAC Synthesis
Azido-PEG1-CH2CO2H is a PROTAC linker, which refers to the alkyl/ether composition. Azido-PEG1-CH2CO2H can be used in the synthesis of PROTAC BRD4 Degrader-1 . Azido-PEG1-CH2CO2H 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.

HY-159777

CPI-203-PEG5-Alkyne		Alkynes
CPI-203-PEG5-Alkyne is a conjugate of E3 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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BRD4-IN-1

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