I-BET151

SKU: orb1226594

Description

I-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor with IC50 of 0.5, 0.25 and 0.79 uM for BRD2, BRD3 and BRD4 in FP assays, shows no effect on the 23 other bromodomain proteins including MLL; demonstrates potent efficacy against cell lines harbouring different MLL-fusions (MOLM13 cell IC50=120 nM, MV4:11 cell IC50=26 nM), induices early cell cycle arrest and apoptosis, selectively abrogates BRD3/4 recruitment to chromatin;shows significant therapeutic value and survival benefit in mouse models of murine MLL-AF9 and human MLL-AF4 leukaemia.

Key Properties

• CAS Number: 1300031-49-5
• MW: 415.4445
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₁N₅O₃
• SMILES: O=C(N1[C@@H](C2=NC=CC=C2)C)NC3=C1C4=CC(OC)=C(C5=C(C)ON=C5C)C=C4N=C3
• Target: Bromodomain
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Animal model: Mice (model of subcutaneous myeloma). Dosage: 50 mg/kg. Administration: i.p.; daily for 21 days. Result: Reduced rate of tumor size doubling than vehicle-treated mice.
• In Vitro:
  Cell Viability Assay Cell line: H929 cells. Concentration: 1 μM. Incubation time: 72 hours. Result: Displays the majority of live cells resided in the G0 phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation. Cell Proliferation Assay Cell line: H929 cells. Concentration: 100 nM. Incubation time: 72 hours. Result: Caused a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK1210151A | I-BET 151 | GSK-1210151A

Quick Database Links

Gene Symbol

Bromodomain