506384 | BLM Helicase Inhibitor, ML216 - Calbiochem

506384
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₁₅H₉F₄N₅OS

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      5.06384.0001
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      Limited AvailabilityLimited Availability
      In Stock 
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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 Image
          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

          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 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.