| Name | Molibresib |
| Description | Molibresib (GSK525762) is an inhibitor of BET proteins (IC50: about 35 nM). |
| Cell Research | CD4+ 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 Assay | Fluorescence 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 vitro | At 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 vivo | At 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). |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 39 mg/mL (92 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.72 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 250 mg/mL (589.76 mM), Sonication is recommended.
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| Keywords | Molibresib | Inhibitor | inhibit | I-BET-762 | I-BET762 | GSK525762A | GSK-525762 | GSK 525762 | EpigeneticReaderDomain | Epigenetic Reader Domain | BET proteins |
| Inhibitors Related | ABBV-744 | SNDX-5613 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | 5-Ph-IAA | Curcumin | dBET6 | Naphthol AS-E | JQ-1 (carboxylic acid) | Bisdemethoxycurcumin |
| Related Compound Libraries | Highly Selective Inhibitor Library | Failed Clinical Trials Compound Library | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
