BML-277

SKU: orb1306692

Description

BML-277

Research Area

Cell Biology

Key Properties

• CAS Number: 516480-79-8
• MW: 363.8
• Purity: 99.63%
• Formula: C₂₀H₁₄ClN₃O₂
• SMILES: NC(=O)c1ccc2nc([nH]c2c1)-c1ccc(Oc2ccc(Cl)cc2)cc1
• Target: Chk,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.75 mM);DMSO:122.5 mg/mL (336.72 mM)

Bioactivity

• Target IC50:
  Chk2:15 nM
• In Vitro:
  BML-277 is an ATP-competitive inhibitor of Chk2 that dose dependently protects human CD4+ and CD8+ T-cells from apoptosis due to ionizing radiation. BML-277 efficiently rescues both T-cell populations from radiation-induced apoptosis in a dose-dependent manner with an observed EC50 of 3 7.6 μM. The concentration of BML-277 required for radioprotection is consistent with the biochemical measurement of chk2 inhibition. Providing theKm of ATP for Chk2 is determined to be 99 μM and the Ki for BML-277 is 37 nM, and assuming that the intracellular ATP concentration is 10 mM, a 5 μM concentration of BML-277 would be expected to produce 42% inhibition of intracellular chk2.
• Cell Research:
  BML-277 is dissolved in DMSO and stored, and then diluted with appropriate medium before use. To determine the radioprotective effect of Chk2 inhibitors, purified T-cells are incubated at 100 000 cells per well in BML-277 (102.5 nM, 1 μM, 100.5 μM, 10 μM, and 101.5 μM) or vehicle (DMSO) at varying concentrations in 96-well stripwells for 1 h. Cells are then exposed to a dose of 0 or 10 Gy gamma irradiation from a 137Cs source at a dose rate of 3.65 Gy/min and then returned to the incubator for a further 24 h. Cells are stained with Annexin V-FITC and propidium iodide, according to the manufacturers protocol. Apoptotic and surviving cells are quantitated with a FACSCalibur FACS machine. Data are reported as percent recovery-or the number of survivors from treatment groups minus the number of cells surviving in the irradiated control group divided by the number of surviving cells in the untreated control groups.

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

Inhibitor, inhibit, Checkpoint Kinase (Chk), Chk2 Inhibitor II, Chk2, Apoptosis, C3742, C-3742, C 3742, BML 277, BML277, BML-277

Compound Identifiers

PubChem CID

9969021