I-BET151

SKU: orb1306440

Description

I-BET151 (GSK1210151A) is a potent and selective small-molecule inhibitor of the BET bromodomain proteins BRD2, BRD3, and BRD4, with reported IC50 values of 0.5, 0.25, and 0.79 μM, respectively, in biochemical assays. It is widely used as a chemical probe in cancer, immunology, and inflammation research, demonstrating activity in both cellular studies and in vivo animal models of leukemia and myeloma.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1300031-49-5
• MW: 415.44
• Purity: 99.63% (May vary between batches)
• Formula: C₂₃H₂₁N₅O₃
• SMILES: Cl.COc1cc2c3n([C@H](C)c4ccccn4)c(=O)[nH]c3cnc2cc1-c1c(C)noc1C
• Target: Epigenetic Reader Domain
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.81 mM);DMSO:50 mg/mL (120.35 mM)

Bioactivity

• Target IC50:
  BRD3:0.25 μM|BRD2:0.5 μM|BRD4:0.79 μM
• In Vivo:
  When interacting with HL60 nuclear extracts, I-BET151 at concentrations of 0.5 or 5 μM inhibits the binding of BETs (BRD2/3/4/9) to acetylated histone peptides without affecting 23 other bromodomain proteins. This compound demonstrates potent inhibitory effects on cell lines with various MLL fusions, such as MV4;11, RS4;11, MOLM13, and NOMO1 cells (IC50: 15-192 nM). I-BET151 shows broad selectivity in inhibiting multiple protein types, including COX-2, P450, Aurora B, GSK3β, PI3K-γ, GPCR, ion channels, and transporters. Similar to I-BET762 (GSK525762A), I-BET151 possesses a high binding affinity for BRD2/3/4 (Kd: 0.02-0.1 μM) and significantly inhibits the production of the IL-6 cytokine in response to lipopolysaccharide stimulation in human peripheral blood mononuclear cells, whole blood, and rat WB (IC50: 0.16/1.26/1.26 μM).
• In Vitro:
  I-BET151 administration (30 mg/kg/day) in mice significantly inhibits the growth of MLL-AF9 murine and MLL-AF4 human leukemia tumors and notably prolongs lifespan.
• Cell Research:
  Cells are exposed to various concentrations of I-BET151 for 24 or 72 hours in 384-well or 96-well plates. For cell growth inhibition assays, plates are added with CellTiter-Glo reagent using a volume equivalent to the cell culture volume in the wells, shaken for approximately 2 minutes and chemiluminescent signal is read on the Analyst GT or EnVision Plate Reader. For cell proliferation assays, CellTiter-Aqueous One is added to each well and plates are incubated for 4 hours at 37 °C. Absorbance is read at 490 nm on a SpectraMax Gemini reader (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.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BRD3, BRD2, BRD4, BET, bromodomain, EpigeneticReaderDomain, Epigenetic Reader Domain, I BET151, I-BET 151, IBET151, I-BET151, I-BET-151, GSK1210151A, Inhibitor, inhibit

Compound Identifiers

PubChem CID

90488961