506384 BLM Helicase Inhibitor, ML216 - Calbiochem

506384
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₅H₉F₄N₅OS

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      Glass bottle 10 mg
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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®
      Synonyms1-(4-Fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea, ML-216
      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
      FormOrange solid
      Hill FormulaC₁₅H₉F₄N₅OS
      Chemical formulaC₁₅H₉F₄N₅OS
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetBLM
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      BLM Helicase Inhibitor, ML216 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Rosenthal, A.S., et al. 2013. Bioorg. Med. Chem. Lett. 23, 5660.
      Nguyen, G.H., et al. 2013. Chem. Biol. 20, 55.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision18-December-2013 JSW
      Synonyms1-(4-Fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea, ML-216
      DescriptionA 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).
      FormOrange solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₅H₉F₄N₅OS
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesRosenthal, A.S., et al. 2013. Bioorg. Med. Chem. Lett. 23, 5660.
      Nguyen, G.H., et al. 2013. Chem. Biol. 20, 55.