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bromodomain BRD4

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (13) Autophagy (3) c-Myc (1) Casein Kinase (1) Drug Derivative (1) Drug Intermediate (2) Drug Isomer (1) Drug Metabolite (1) E3 Ligase Ligand-Linker Conjugates (1) Epigenetic Reader Domain (102) ERK (3) Fluorescent Dye (1) HDAC (1) Histone Acetyltransferase (8) HSP (1) Interleukin Related (1) Ligands for Target Protein for PROTAC (3) Molecular Glues (6) NF-κB (1) Parasite (1) PARP (1) PD-1/PD-L1 (1) Polo-like Kinase (PLK) (2) PROTACs (9) Reference Standards (5) STAT (1)
By Research Areas:	Cancer (92) Cardiovascular Disease (1) Infection (1) Inflammation/Immunology (16) Metabolic Disease (1) Neurological Disease (3)
Click Chemistry:	PROTAC Synthesis (1) Tetrazine (1) Alkynes (1)

110

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Isotope-Labeled Compounds

Antibodies

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13030

(+)-JQ-1 Maximum Cited Publications 295 Publications Verification JQ1	Epigenetic Reader Domain Autophagy Ligands for Target Protein for PROTAC	Neurological Disease Cancer
(+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, CNS-penetrant and reversible BET bromodomain inhibitor, with IC₅₀s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)) . (+)-JQ-1 also activates autophagy .

HY-111784

Inobrodib 10+ Cited Publications CCS1477	Epigenetic Reader Domain	Cancer
Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with K_d values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a K_d of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression .

HY-15826

SGC-CBP30 15+ Cited Publications	Epigenetic Reader Domain Histone Acetyltransferase	Inflammation/Immunology Cancer
SGC-CBP30, a chemical probe, is a potent and highly selective CBP/p300 bromodomain (K_ds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of **BRD4 [BRD4(1)]** bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects .

HY-78695

JQ-1 carboxylic acid 5+ Cited Publications	Epigenetic Reader Domain PD-1/PD-L1 Ligands for Target Protein for PROTAC	Cancer
JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of *BRD4*.

HY-13235

I-BET151 25+ Cited Publications GSK1210151A	Epigenetic Reader Domain	Cancer
I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits *BRD4, BRD2, and BRD3* with pIC₅₀ of 6.1, 6.3, and 6.6, respectively .

HY-100015

Mivebresib 10+ Cited Publications ABBV-075	Epigenetic Reader Domain Apoptosis	Cancer
Mivebresib (ABBV-075) is a potent and orally active **bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a K_i** of 1.5 nM .

HY-136570

GSK778 1 Publications Verification iBET-BD1	Epigenetic Reader Domain Apoptosis	Inflammation/Immunology Cancer
GSK778 (iBET-BD1), a chemical probe, 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-15846

CPI-203 5+ Cited Publications	Epigenetic Reader Domain Apoptosis	Cancer
CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC₅₀ value of appr 37 nM (BRD4 α-screen assay).

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-100653A

AZD5153 6-Hydroxy-2-naphthoic acid 5 Publications Verification	Epigenetic Reader Domain	Cancer
AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available *BET/BRD4* bromodomain inhibitor; disrupts BRD4 with an IC₅₀ of 1.7 nM.

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-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-151594

iBRD4-BD1	Epigenetic Reader Domain	Inflammation/Immunology Cancer
iBRD4-BD1 is selective **BRD4 bromodomain** inhibitor. iBRD4-BD1 has inhibition activity for BRD4 bromodomain with an IC₅₀ value of 12 nM. iBRD4-BD1 can be used for the research of inflammation and oncology .

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-15658

GSK2801 3 Publications Verification	Epigenetic Reader Domain Apoptosis	Cancer
GSK2801, a chemical probe, is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with K_d values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4 .

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-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-136857

BRD4 degrader-3	Epigenetic Reader Domain	Cancer
BRD4 degrader-3 is a potent **bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC₅₀*s 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 .

HY-16586

PFI-1 3 Publications Verification	Epigenetic Reader Domain Autophagy Apoptosis	Cancer
PFI-1, a chemical probe, is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC₅₀ of 0.22 μM in a cell-free assay.

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-134463

NHWD-870 1 Publications Verification	Epigenetic Reader Domain Apoptosis	Cancer
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC₅₀=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .

HY-120028

GNE-207	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC₅₀ of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC₅₀ of 18 nM for MYC expression in MV-4-11 cells .

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-128341

ERK5-IN-2	ERK	Cardiovascular Disease Cancer
ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC₅₀s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis .

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-112375

AT6	PROTACs	Cancer
AT6 is a PROTAC AT1 analogue, which is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4* with highly selectivity to bromodomain (Brd4).

HY-117286

(S)-JQ-35 TEN-010	Epigenetic Reader Domain Apoptosis	Neurological Disease Cancer
(S)-JQ-35 (TEN-010) is an orally active, blood-brain barrier-permeable bromodomain inhibitor that selectively targets the bromodomain and extra-terminal domain (BET) protein family (BRD4, BRD3, BRD2 and BRDT). (S)-JQ-35 blocks the activation of Myc gene expression by BRD4, thereby inhibiting cancer cell proliferation and promoting cancer cell apoptosis. (S)-JQ-35 can be used in research related to NUT midline carcinoma and neuroblastoma .

HY-156214

NICE-01 AP1867-PEG2-JQ1; AP-PEG2-JQ1	Epigenetic Reader Domain	Others
NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound that bind to proteins in separate cellular compartments that can induce nuclear import of cytosolic cargoes, using nuclear-localized bromodomain-containing protein 4 (BRD4) as a “carrier” for co-import and nuclear trapping of cytosolic proteins .

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-131061

BET bromodomain inhibitor 1	Epigenetic Reader Domain	Cancer
BET bromodomain inhibitor 1 is an orally active, selective **bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC₅₀** of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (K_d values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity .

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-160528

IBG3 1 Publications Verification	Epigenetic Reader Domain Molecular Glues	Cancer
IBG3 is a Molecular glue degrader targeting *BRD2* and *BRD4, with DC₅₀* values of 8.6 pM and 6.7 pM, respectively. IBG3 binds simultaneously to the tandem bromodomains of BRD2/BRD4, induces intramolecular conformational changes, enhances the affinity of BRD2/BRD4 for DCAF16, and promotes ubiquitination and degradation. IBG3 is applicable to the research of chronic myeloid leukemia .

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-103036

BET bromodomain-IN-5	Epigenetic Reader Domain Apoptosis	Cancer
BET bromodomain-IN-5 is an orally active BET inhibitor with an IC₅₀ of 14 nM against *BRD4* (1). BET bromodomain-IN-5 can inhibit the proliferation of tumor cells and induce cell cycle arrest and apoptosis. BET bromodomain-IN-5 can be used in the research of tumors .

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-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-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-124596

CD161	Epigenetic Reader Domain	Cancer
CD161 is a potent, selective and orally bioavailable **bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC₅₀*s of 28.2 nM and 7.2 nM for BRD4* BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity .

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-111502

Y06036	Epigenetic Reader Domain	Cancer
Y06036 is a potent and selective BET inhibitor, which binds to the *BRD4(1)* bromodomain with K_d value of 82 nM . Antitumor activity .

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-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-136920

CBP/p300-IN-8 1 Publications Verification	Epigenetic Reader Domain	Cancer
CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 family of bromodomains. CBP/p300-IN-8 inhibits CBP (IC₅₀=0.01-0.1 µΜ) and BRD4 (IC₅₀=1-1000 µΜ) activity .

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 .

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-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-111916

ODM-207 BET-IN-4	Epigenetic Reader Domain	Cancer
ODM-207 (BET-IN-4) is a potent BET bromodomain protein (BRD4) inhibitor, with an IC₅₀ of ≤ 1 μM .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N3213

Naringenin triacetate	Flavonoids Classification of Application Fields Flavonones Rutaceae Plants Disease Research Fields Citrus Cancer Source Classification	Epigenetic Reader Domain
Naringenin triacetate is a flavonoid isolated from plant, exhibits a good binding affinity with multiple crystal structures of first bromodomain BRD4 (BRD4 BD1) .

Cat. No.	Compare	Product Name	Species	Source	Image

HY-P7846

	BRD4 Protein, Human (His-Flag) 3 Publications Verification rHubromodomain-containing protein 4/BRD4, His-Flag; HUNK1; HUNK1bromodomain-containing protein 4; HUNKI; MCAP	Human	E. coli
	The BRD4 protein is a chromatin reader that recognizes and binds acetylated histones, transmits epigenetic memory and regulates transcription during cell division. It associates with acetylated chromatin throughout the cell cycle, maintaining chromatin structure and contributing to epigenetic memory. BRD4 Protein, Human (His-Flag) is the recombinant human-derived BRD4 protein, expressed by E. coli , with N-10*His, N-Flag labeled tag.

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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 .

Host:	Rabbit (2)
Reactivity:	Human (2) Rat (2) Mouse (2)
Application:	IHC-P (2) ICC/IF (2) IP (2) WB (2)
Isotype:	IgG (2)
Conjugation:	Non-conjugated (2)
Clonality:	Monoclonal (1) Recombinant (1)
Modification:	Unmodified (1)

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HY-P80976

	BRD4 Antibody (YA3486) 1 Publications Verification BRD4; CAP; HUNK1; MCAP; bromodomain containing 4; chromosome associated protein	WB, IHC-P, ICC/IF, IP	Human, Mouse, Rat
	BRD4 Antibody (YA3486) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to BRD4.

HY-P80976A

	BRD4 Antibody (YA3486)(PBS only) BRD4; CAP; HUNK1; MCAP; bromodomain containing 4; chromosome associated protein	WB, IHC-P, ICC/IF, IP	Human, Mouse, Rat
	BRD4 Antibody (YA3486) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to BRD4.

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HY-136857

BRD4 degrader-3		PROTAC Synthesis
BRD4 degrader-3 is a potent **bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC₅₀*s 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-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-182371

BRD4 ligand 15		Alkynes
BRD4 ligand 15 (compound 5) is a BRD4 ligand and alkyne-modified chalcone derivative, which serves as a building block for the synthesis of BRD4-targeting PROTAC TKP-5 (HY-182370) .

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bromodomain BRD4

Inhibitors & Agonists

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Biochemical Assay Reagents

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