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Results for "

BRD4 inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (5) AMPK (2) Androgen Receptor (4) Apoptosis (46) Autophagy (5) Bcl-2 Family (3) Btk (1) c-Fms (1) c-Myc (14) CaMK (1) Casein Kinase (2) Caspase (3) CDK (6) Discoidin Domain Receptor (1) DNA-PK (2) DNA/RNA Synthesis (7) Drug Derivative (1) Drug Intermediate (2) Drug Isomer (2) Drug Metabolite (1) E3 Ligase Ligand-Linker Conjugates (2) EGFR (1) Epigenetic Reader Domain (250) ERK (3) FGFR (1) FKBP (2) FLT3 (1) HDAC (4) Histone Acetyltransferase (16) Histone Methyltransferase (1) HIV (4) HSP (1) HyT (1) Interleukin Related (4) JAK (2) Ligands for Target Protein for PROTAC (19) MDM-2/p53 (2) Molecular Glues (3) mTOR (1) NAMPT (1) Necroptosis (1) NF-κB (3) p38 MAPK (1) PAK (2) Parasite (1) PARP (4) PD-1/PD-L1 (3) PDGFR (1) Phosphatase (1) PI3K (9) Polo-like Kinase (PLK) (6) PROTAC-Linker Conjugates for PAC (1) PROTACs (26) Reactive Oxygen Species (ROS) (3) Reference Standards (10) RET (1) RIP kinase (1) ROS Kinase (1) SARS-CoV (1) Src (1) STAT (3) Survivin (1) TNF Receptor (2) TNK1 (1)
By Research Areas:	Cancer (225) Cardiovascular Disease (3) Endocrinology (1) Infection (8) Inflammation/Immunology (48) Metabolic Disease (3) Neurological Disease (9)
Click Chemistry:	PROTAC Synthesis (1) Tetrazine (1) Alkynes (2)

265

Inhibitors & Agonists

Fluorescent Dyes

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

GMP Molecules

Targets Recommended: Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-100653

AZD5153 5 Publications Verification	Epigenetic Reader Domain Apoptosis	Cancer
AZD5153 is a bivalent, selective, and orally active *BET/BRD4* bromodomain inhibitor with an IC₅₀ of value of 5 nM for full-length BRD4 (FL-BRD4). AZD5153 ligates two bromodomains in BRD4 simultaneously. AZD5153 can be used for the study of cancer, such as acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma .

HY-114305

A1874 2 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
A1874 is a nutlin-based (MDM2 ligand) and *BRD4*-degrading PROTAC with a DC₅₀ of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation .

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-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-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-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-117997

UMB-32	Epigenetic Reader Domain	Cancer
UMB-32, a potent, selective *BRD4* inhibitor, binds BRD4 with the K_d of 550 nM, and IC₅₀ of 637 nM. UMB-32 also shows potency against TAF1, a bromodomain-containing transcription factor .

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-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-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-145260

BRD4/CK2-IN-1	Epigenetic Reader Domain Casein Kinase Apoptosis Autophagy	Cancer
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of *BRD4/CK2* (bromodomain-containing protein 4/casein kinase 2), with IC₅₀s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)

HY-158031

PLK1/BRD4-IN-5	Apoptosis Polo-like Kinase (PLK) Epigenetic Reader Domain	Cancer
PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and *BRD4* inhibitor with IC₅₀ values of 0.3  nM and 60.8  nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research .

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-131203

PROTAC BRD4 Degrader-6	PROTACs Epigenetic Reader Domain Caspase Apoptosis c-Myc	Cancer
PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule *BRD4*PROTAC degrader with IC₅₀ value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research .

HY-156566

PROTAC BRD4 Degrader-21	PROTACs Epigenetic Reader Domain HSP	Cancer
PROTAC BRD4 Degrader-21 is a *BRD4*-targeting PROTAC degrader with an IC₅₀ value of 59 nM. PROTAC BRD4 Degrader-21 induces ubiquitination of *BRD4, leading to its degradation via the proteasome. PROTAC BRD4* Degrader-21 binds to recombinant HSP90α protein with moderate affinity, having an IC₅₀ of 100-1000 nM. PROTAC BRD4 Degrader-21 induces cancer cell death. PROTAC BRD4 Degrader-21 inhibits tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-21 can be used for the research of acute myeloid leukemia, diffuse large B-cell lymphoma .

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-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-132130

BRD4 Inhibitor-13	Epigenetic Reader Domain	Inflammation/Immunology Cancer
BRD4 Inhibitor-13 (Compound 2) is a *BRD4* ligand, and can be used for research of cancer, inflammation.

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-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. PROTAC BRD2/BRD4 degrader-1 effectively inhibits solid tumors with low cytotoxic effect .

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-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-174811

PROTAC BRD4 Degrader-33	PROTACs Epigenetic Reader Domain PD-1/PD-L1	Inflammation/Immunology Cancer
PROTAC BRD4 Degrader-33 is an enzyme activated clickable *BRD4* PROTAC degrader with favorable tumor microenvironment-response. PROTAC BRD4 Degrader-33 has superior tumor tissue penetration capabilities and efficiently inhibits PD-L1 protein expression. PROTAC BRD4 Degrader-33 shows potent anti-tumoral immunomodulation activity in 4T1 tumor-bearing mice model . Pink: BRD4 ligand (HY-174812); Blue: CRBN ligase ligand (HY-10984); Black: linker

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-160499

BRD4 Inhibitor-30	Epigenetic Reader Domain	Cancer
BRD4 inhibitor-30 (Compound 1) is a *BRD4* inhibitor with a IC₅₀ value of 415 nM .

HY-143235

BRD4 Inhibitor-15	Epigenetic Reader Domain Apoptosis Bcl-2 Family Caspase c-Myc	Cancer
BRD4 Inhibitor-15 (compound 13) is a potent *BRD4* inhibitor, with an IC₅₀ of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .

HY-174088

CDK4/6/BRD4-IN-2	CDK Discoidin Domain Receptor Apoptosis Reactive Oxygen Species (ROS) DNA/RNA Synthesis	Cancer
CDK4/6/BRD4-IN-2 (Compound PJ2) is a dual inhibitor of CDK4/6 and *BRD4* with IC₅₀ values for CDK4, CDK6, BRD4 (BD1), and BRD4 (BD2) of 168.75, 292.45, 23.17, and 3.12 nM respectively. CDK4/6/BRD4-IN-2 has a strong inhibitory effect on non-small cell lung cancer (NSCLC) cell lines. CDK4/6/BRD4-IN-2 induces cell cycle arrest, senescence and apoptosis through ROS-mediated DNA damage. CDK4/6/BRD4-IN-2 can also effectively inhibit the migration and invasion of NCI-H358 cells. CDK4/6-IN-2 can be used for the study of KRAS-mutated NSCLC .

HY-174812

BRD4 ligand 8	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Inflammation/Immunology Cancer
BRD4 ligand 8 (Compound J558) is a *BRD4* inhibitor. BRD4 ligand 8 can be used for synthesis of PROTAC BRD4 Degrader-33 (HY-174811) .

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-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-153751

BRD4-IN-4	Epigenetic Reader Domain	Cancer
BRD4-IN-4 (Compound 1) is a *BRD4* inhibitor (IC₅₀=6.83 μM). BRD4-IN-4 selectively inhibits MV4-11 cell line proliferation and arrests cell at G1 phase. BRD4-IN-4 can be used for research of MLL leukemia .

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-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-173564

DW34	Epigenetic Reader Domain Necroptosis	Inflammation/Immunology
DW34 is an orally active pan-BRD4-D1 biased inhibitor with additional BRD4-D2 inhibitive activity. DW34 displays comparable inhibitive efficacy to I-BET151 (HY-13235) (EC₅₀ = 0.16 μM) with low nanomolar EC₅₀ values of 0.14 μM. DW34 significantly reduces liver inflammation induced by LPS (HY-D1056) and APAP (HY-66005) via reducing chemokine expression and cellular necrosis .

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-175767

PROTAC BRD4 Degrader-39	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-39 is a selective targeting Bromodomain protein 4 (BRD4) degrader with an DC₅₀ value of 24.66 nM. PROTAC BRD4 Degrader-39 conjugates BRD PROTAC (ARV-771) (HY-100972) with carbohydrate. PROTAC BRD4 Degrader-39 selectively delivers to tumor cells with high GLUT1 expression, followed by GSH-triggered release of ARV-771 and degrades BRD4. PROTAC BRD4 Degrader-39 can inhibit tumor growth and show no significant toxicity. PROTAC BRD4 Degrader-39 can be used for the research of cancer, such as breast cancer . (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: (HY-42427); BRD4 ligand-Linker: (HY-42429))

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-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-176521A

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

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-157290

HL403	Epigenetic Reader Domain Src	Cancer
HL403 is a potent and dual *BRD4/Src* inhibitor. HL403 has IC₅₀ values of 133 nM for BRD4 inhibition and 4.5 nM for Src inhibition. HL403 shows anti-cancer activity .

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-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-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-160670

BRD4-IN-6	Epigenetic Reader Domain	Cancer
BRD4-IN-6 (compound 116) is a *BRD4* inhibitor (extracted from patent CN107721975A).

Cat. No.	Product Name	Type

HY-50698G

BI 2536	Biochemical Assay Reagents
BI 2536 (GMP) is BI 2536 (HY-50698) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BI 2536 is a dual PLK1 and *BRD4* inhibitor with IC₅₀s of 0.83 and 25 nM, respectively . BI-2536 suppresses IFNB (encoding IFN-β) gene transcription .

HY-78197

3,5-Dimethylisoxazole-4-boronic acid pinacol ester	Biochemical Assay Reagents
3,5-Dimethylisoxazole-4-boronic acid pinacol ester is a drug intermediate that can be used for the synthesis of bromodomain inhibitors .

Cat. No.	Product Name	Target	Research Area

HY-P10446

TAT-PiET-PROTAC	Epigenetic Reader Domain PROTACs	Cancer
TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of *BRD4. TAT-PiET-PROTAC can reduce BRD4* and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer .

HY-P10445

TAT-PiET	Epigenetic Reader Domain	Cancer
TAT-PiET is a cell-penetrating peptide targeting the extra-terminal (ET) domain of *BRD4. TAT-PiET can reduce BRD4* and JMJD6 levels and inhibit cell proliferation. TAT-PiET also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET can be used for the research of cancer, such as breast cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2000

Bellidifolin 1 Publications Verification	Infection Structural Classification Xanthones Classification of Application Fields Swertia bimaculata (Sieb. et Zucc.) Hook. f. et Thoms. ex C. B. Clark Gentianaceae Phenols Polyphenols Plants Inflammation/Immunology Disease Research Fields Source Classification	STAT PI3K mTOR Akt
Bellidifolin is an orally active compound with antiproliferative, anti-inflammatory and antioxidant properties. Bellidifolin modulates key signaling pathways including STAT3, PI3K-Akt, mTOR and *BRD4, and inhibits* the viral protein R (Vpr). Bellidifolin induces cell cycle arrest and apoptosis, exerts significant antifibrotic effects, and protects the heart, liver and nervous system. Bellidifolin is applicable to the research of various diseases such as lung cancer, non-alcoholic fatty liver disease, myocardial hypertrophy and ischemic cranial nerve injury .

HY-N16067

Penipanoid C	Alkaloids Marine natural products Quinoline Alkaloids Marine microorganism Source Classification	Epigenetic Reader Domain
Penipanoid C (Compound 9) is a *BRD4* inhibitor. Penipanoid C can be isolated from marine sediment-derived fungus Penicillium paneum SD-44. Penipanoid C has anti-inflammatory activity and cytotoxic activity against the SMMC-7721 cells. Penipanoid C can be used for inflammatory diseases research .

HY-177139

CDD-1349	other families Phenols Polyphenols Plants Pteris multifida Poir. Source Classification	Epigenetic Reader Domain
CDD-1349 (Compound 15) is a *BRDT-BD2/BRD4-BD2* selective inhibitor. CDD-1349is an analog with sixfold selectivity for BRDT-BD2 versus BRD4-BD2. CDD-1349 has an IC₅₀ of 22 nM against BRDT. CDD-1349 can be studied in research on nonhormonal contraceptive agent .

HY-N15522

Bi-magnolignan	Magnoliaceae Houpoea officinalis (Rehder & E. H. Wilson) N. H. Xia & C. Y. Wu Phenols Polyphenols Plants Source Classification	Epigenetic Reader Domain
Bi-magnolignan is a *BRD4* inhibitor that induces DNA damage and apoptosis. Bi-magnolignan inhibits HCT116 cell proliferation with an IC₅₀ value of 2.9 μM .

Cat. No.	Product Name	Chemical Structure

HY-150516S

BET-IN-12
BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC₅₀ of 0.9 nM for BRD4 .

Cat. No.	Product Name		Classification

HY-101460

Tz-Thalidomide		Tetrazine
Tz-Thalidomide is a tetrazine-tagged Thalidomide (HY-14658), an E3 ligase ligand. Tz-Thalidomide self-assembles with TCO-labeled target protein inhibitors, forming a CLIP-TAC (targeted protein degradation chimera) via click chemistry. This chimera recruits the E3 ubiquitin ligase CRBN to the target protein, thereby inducing ubiquitination and subsequent degradation of the target protein. When used in combination with JQ1-TCO (HY-148864), Tz-Thalidomide induces concentration-dependent degradation of *BRD4* in cells. When combined with ERK-targeting protein inhibitors, Tz-Thalidomide induces degradation of ERK1/2 in cells. Tz-Thalidomide can be used in cancer-related research .

HY-44103

Desmethyl-QCA276 PROTAC BRD4-binding moiety 4		PROTAC Synthesis
Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC₅₀ of 10 nM, and with a K_i of 2.3 nM . Desmethyl-QCA276 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-176502

FKBP12 ligand-3		Alkynes
FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. FKBP12 ligand-3 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-3 can be used for selective cancer research based on differences in intracellular presenter protein levels .

HY-176501

FKBP12 ligand-2		Alkynes
FKBP12 ligand-2 (compound d) is a high affinity ligand targeting FKBP12. FKBP12 ligand-2 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-2 can be used for selective cancer research based on differences in intracellular presenter protein levels .

Targets Recommended: Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-50698G

BI 2536	Polo-like Kinase (PLK) Apoptosis Epigenetic Reader Domain	Cancer
BI 2536 (GMP) is BI 2536 (HY-50698) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BI 2536 is a dual PLK1 and *BRD4* inhibitor with IC₅₀s of 0.83 and 25 nM, respectively . BI-2536 suppresses IFNB (encoding IFN-β) gene transcription .

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