509667 VprBP Inhibitor, B32B3 - Calbiochem

509667
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₉H₁₇N₅S

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      Glass bottle 10 mg
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      Description
      OverviewA cell permeable, potent, selective, and ATP-competitive inhibitor of Vpr (HIV-1) binding protein (VprBP) that preferentially targets cancer cells expressing VprBP and blocks phosphorylation of H2A at Thr120 (IC50 = 500 nM in DU-145 human prostate cancer cells) and reduces cell proliferation. However, it has minimal effect on normal human prostate MLC cells lacking VprBP. Exhibits over 100-fold greater selectivity for VprBP over a panel of 33 other protein kinases. Shown to reduce xenograft tumor progression in nude mice injected with DU-145 cells (~5 mg/kg, i.p. twice a week for 3 weeks). Displays moderately desirable pharmacokinetic properties with t1/2= 7 h and Cmax of 1 µM.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number509667
      Brand Family Calbiochem®
      SynonymsVpr Binding protein Inhibitor
      References
      ReferencesKim, K., et al. 2013. Mol. Cell. 52, 459.
      Product Information
      FormLight yellow powder
      Hill FormulaC₁₉H₁₇N₅S
      Chemical formulaC₁₉H₁₇N₅S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetVprBP
      Primary Target IC<sub>50</sub>500 nM
      Purity≥98% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      VprBP Inhibitor, B32B3 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Kim, K., et al. 2013. Mol. Cell. 52, 459.
      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-April-2014 JSW
      SynonymsVpr Binding protein Inhibitor
      DescriptionA cell permeable, potent, selective, and ATP-competitive inhibitor of Vpr (HIV-1) binding protein (VprBP) that preferentially targets cancer cells expressing VprBP and blocks phosphorylation of H2A at Thr120 (IC50 = 500 nM in DU-145 human prostate cancer cells) and reduces cell proliferation. However, it has minimal effect on normal human prostate MLC cells lacking VprBP. Exhibits over 100-fold greater selectivity for VprBP over a panel of 33 other protein kinases. Shown to reduce xenograft tumor progression in nude mice injected with DU-145 cells (~5 mg/kg, i.p. twice a week for 3 weeks). Displays moderately desirable pharmacokinetic properties with t1/2= 7 h and Cmax of 1 µM.
      FormLight yellow powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₉H₁₇N₅S
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (50 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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesKim, K., et al. 2013. Mol. Cell. 52, 459.