Molibresib

SKU: orb1307159

Description

Molibresib (GSK525762) is a potent and selective BET bromodomain inhibitor with an IC50 of approximately 35 nM. It is widely used in cancer research, demonstrating activity in both in vitro assays and in vivo models for studying oncology and transcriptional regulation.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1260907-17-2
• MW: 423.9
• Purity: 98.82%
• Formula: C₂₂H₂₂ClN₅O₂
• SMILES: CCNC(=O)C[C@@H]1N=C(c2ccc(Cl)cc2)c2cc(OC)ccc2-n2c(C)nnc12
• Target: Epigenetic Reader Domain
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:60 mg/mL (141.54 mM);Ethanol:39 mg/mL (92 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.72 mM)

Bioactivity

• Target IC50:
  BET proteins:35 nM
• In Vivo:
  At day 2 of differentiation, I-BET-762 treatment altered cytokine production in CD4+ T cells, up-regulatin the expression of some anti-inflammatory gene products and down-regulatin the expression of some pro-inflammatory cytokines.I-BET-762 inhibite the binding of bromodomain and additional terminal domain proteins and BRD2/3/4 to the andem bromodomain o the BET (Kd: 50.5-61.3 nM). In FRET analysis, displacement o the BET andem bromodomain a tetraacetylated H4 peptide IC50 32.5-42.5 nM).
• In Vitro:
  At day 2 of differentiation, I-BET-762 treatment altered cytokine production in CD4+ T cells, up-regulatin the expression of some anti-inflammatory gene products and down-regulatin the expression of some pro-inflammatory cytokines.I-BET-762 inhibite the binding of bromodomain and additional terminal domain proteins and BRD2/3/4 to the andem bromodomain o the BET (Kd: 50.5-61.3 nM). In FRET analysis, displacement o the BET andem bromodomain a tetraacetylated H4 peptide IC50 32.5-42.5 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 durin the 60–72 h of initial activation. Ove the course of 5 d of T-cell culture and expansion the compounds is diluted 12-fold relative to the starting concentration .(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Molibresib, Inhibitor, inhibit, I-BET 762, I-BET762, I-BET-762, GSK-525762, GSK525762A, GSK525762, GSK 525762, GSK 525762A, EpigeneticReaderDomain, Epigenetic Reader Domain, BET proteins

Compound Identifiers

PubChem CID

46943432