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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Epigenetics>Epigenetic Reader Domain inhibitors>Molibresib
Molibresib
  • Molibresib

Molibresib NEW

Price $36 $52 $85
Package 1mg 2mg 5mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Molibresib CAS No.: 1260907-17-2
Purity: 99.08% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameMolibresib
DescriptionMolibresib (GSK525762) is an inhibitor of BET proteins (IC50: about 35 nM).
Cell ResearchCD4+ T cells are isolated from lymph nodes and spleens of 10- to 12-wk old mice and activated with plate bound anti-CD3 and anti-CD28 antibodies in the presence of indicated cytokines. I-BET-762 compounds is included during the 60–72 h of initial activation. Over the course of 5 d of T-cell culture and expansion, the compounds is diluted 12-fold relative to the starting concentrations.(Only for Reference)
Kinase AssayFluorescence resonance energy transfer (FRET) titrations: Fluorescence resonance energy transfer (FRET) titrations. I-BET is titrated against BRD2 (200 nM), BRD3 (100 nM) and BRD4 (50 nM) in 50 mM HEPES pH7.5, 50 mM NaCl, 0.5 mM CHAPS in the presence of tetra-acetylated Histone H4 peptide (200 nM). After equilibrating for 1 hour, the bromodomain protein : peptide interaction is detected using FRET following the addition of 2 nM Europium cryptate labelled streptavidin and 10 nM XL-665-labelled anti-6His antibody in assay buffer containing 0.05% (v/v) BSA and 400 mM KF. Plates are read using an Envision Plate reader (excitation 320 nm, emission 615 nm and 665 nm).
In vitroAt day 2 of differentiation, I-BET-762 treatment altered cytokine production in CD4+ T cells, up-regulating the expression of some anti-inflammatory gene products and down-regulating the expression of some pro-inflammatory cytokines.I-BET-762 inhibited the binding of bromodomain and additional terminal domain proteins and BRD2/3/4 to the tandem bromodomain of the BET (Kd: 50.5-61.3 nM). In FRET analysis, displacement of the BET tandem bromodomain a tetraacetylated H4 peptide (IC50: 32.5-42.5 nM).
In vivoAt day 2 of differentiation, I-BET-762 treatment altered cytokine production in CD4+ T cells, up-regulating the expression of some anti-inflammatory gene products and down-regulating the expression of some pro-inflammatory cytokines.I-BET-762 inhibited the binding of bromodomain and additional terminal domain proteins and BRD2/3/4 to the tandem bromodomain of the BET (Kd: 50.5-61.3 nM). In FRET analysis, displacement of the BET tandem bromodomain a tetraacetylated H4 peptide (IC50: 32.5-42.5 nM).
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationEthanol : 39 mg/mL (92 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 60 mg/mL (141.54 mM)
KeywordsGSK525762A | Inhibitor | inhibit | GSK-525762 | I-BET-762 | Epigenetic Reader Domain | I-BET762 | Molibresib | GSK 525762
Inhibitors RelatedABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Anacardic Acid | Curcumin | dBET6 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin | GSK1379725A
Related Compound LibrariesHighly Selective Inhibitor Library | Reprogramming Compound Library | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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