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506384 BLM Helicase Inhibitor, ML216 - CAS 1430213-30-1 - Calbiochem

Overview

Key Spec Table

CAS #Empirical Formula
1430213-30-1C₁₅H₉F₄N₅OS

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      Description
      OverviewA cell-permeable pyridinyl-thiadiazolylurea compound that selectively blocks Bloom′s syndrome protein (BLM) helicase activity of both full-length as well as truncated BLM636-1298 forms (IC50 = 2.98 and 0.97 µM, respectively). Competes with and reversibly blocks DNA binding to BLM. However, the inhibition appears to be non-competitive with respect to ATP. Exhibits anti-proliferative activity in cells expressing BLM, but not in those lacking BLM. Induces sister chromatid exchanges (SCEs) and enhances the sensitivity of BLM containing PSNF5 cells to aphidicolin (Cat. No. 178273) without affecting PSNG13 cells that are devoid of BLM. Displays favorable microsomal (T1/2 > 1.2 h) and plasma stability (~100% at 5 h).
      Catalogue Number506384
      Brand Family Calbiochem®
      SynonymsML-216, 1-(4-Fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea
      References
      ReferencesRosenthal, A.S., et al. 2013. Bioorg. Med. Chem. Lett. 23, 5660.
      Nguyen, G.H., et al. 2013. Chem. Biol. 20, 55.
      Product Information
      CAS number1430213-30-1
      FormOrange solid
      Hill FormulaC₁₅H₉F₄N₅OS
      Chemical formulaC₁₅H₉F₄N₅OS
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetBLM
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      5.06384.0001CN 04055977243284