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BML-277

BML-277

Catalog Number:
L002369876APE
Mfr. No.:
APE-B1236
Price:
$241
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      • Overview

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          Background

          BML-277 is novel, potent and highly selective inhibitor of the chk2 with the IC50 value of 15±6.9nM [1].BML-277 has shown the ATP-competitive inhibition of chk2 with the Ki value of 37nM. BML-277 has also been exhibited to be a chk2 inhibitor with the IC50 value of 15±6.9nM and efficiently rescue T-cell populations from the apoptosis of radiation-induced in a concentration-dependent fashion with the EC50 of 3~7.6μM. The Km of ATP for chk2 is 99μM and assuming that intracellular ATP concentration is 10mM. Apart from these, BML-277 has shown the inhibition through docking into a homology model of chk2 ATP binging site [1].

          [1]Arienti KL1, Brunmark A, Axe FU, McClure K, Lee A, Blevitt J, Neff DK, Huang L, Crawford S, Pandit CR, Karlsson L, Breitenbucher JG. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85.

      • Properties
        • Alternative Name
          2-[4-(4-chlorophenoxy)phenyl]-3H-benzimidazole-5-carboxamide
          CAS Number
          516480-79-8
          Molecular Formula
          C20H14ClN3O2
          Molecular Weight
          363.8
          Appearance
          A solid
          Purity
          99.75%
          Solubility
          insoluble in H2O; ≥18.2 mg/mL in DMSO; ≥2.72 mg/mL in EtOH with ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference

        • 1. Zheng K, Ma J, et al. "Sulforaphane Inhibits Autophagy and Induces Exosome-Mediated Paracrine Senescence via Regulating mTOR/TFE3." Mol Nutr Food Res. 2020;e1901231. PMID:32476238
          2. Sarkar R, Patra U, et al. "Rotavirus activates a noncanonical ATM-Chk2 branch of DNA damage response during infection to positively regulate viroplasm dynamics." Cell Microbiol. 2019 Dec 17:e13149. PMID:31845505
          3. N. Sanjib Banerjee, Dianne Moore, et al. "Targeting DNA Damage Response as a Strategy to Treat HPV Infections." Int. J. Mol. Sci. 2019, 20(21), 5455.

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