Search Result

Results for "

BRD4-BD1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AMPK (1) Apoptosis (9) Bcl-2 Family (1) c-Myc (3) Caspase (1) CDK (1) Epigenetic Reader Domain (67) Histone Acetyltransferase (2) HIV (1) Interleukin Related (1) Ligands for Target Protein for PROTAC (1) p38 MAPK (1) PAK (1) PI3K (2) Polo-like Kinase (PLK) (1) PROTACs (13) TNF Receptor (1)
By Research Areas:	Cancer (58) Cardiovascular Disease (1) Infection (2) Inflammation/Immunology (15)
Click Chemistry:	PROTAC Synthesis (1)

Inhibitors & Agonists

Natural
Products

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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-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-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-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-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-123844

dBET57 3 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-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-172130

PI3Kδ/BET-IN-1	PI3K Epigenetic Reader Domain	Cancer
PI3Kδ/BET-IN-1 (compound 10b) shows excellent and balanced activities against PI3Kδ (IC₅₀ = 112 nM) and BRD4-BD1 (IC₅₀ = 19 nM) and exhibits strong antiproliferative activities in DLBCL cells .

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-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-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-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-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-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-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-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-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-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-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-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-W265951

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

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-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-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-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-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-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-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-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-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-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-136570A

GSK778 hydrochloride iBET-BD1 hydrochloride	Apoptosis Epigenetic Reader Domain	Inflammation/Immunology Cancer
GSK778 (iBET-BD1) hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC₅₀s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), 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-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-100482

CPI-637 Maximum Cited Publications 12 Publications Verification	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-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-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-136570

GSK778 iBET-BD1	Epigenetic Reader Domain Apoptosis	Inflammation/Immunology Cancer
GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC₅₀s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models .

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 .

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.

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

BRD4-BD1

Inhibitors & Agonists

NaturalProducts

Click Chemistry

Natural
Products