385570 Heat Shock Factor 1 Inhibitor, KRIBB11 - Calbiochem

385570
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₃H₁₂N₆O₂

Pricing & Availability

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385570-10MG
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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable 2,6-diaminopyridine compound that interacts with HSF1 in a reversible manner and prevents HSF1 from recruiting p-TEFb to the hsp70 promoter site (IC50 ≤3 µM in HCT-116 ChIP assays), a critical step for heat shock-induced transcription activation (IC50 <1, <3, <5, and <10 µM, respectively, against reporter, HSP47, HSP27, and HSP70 transcription in HCT-116 cultures). Reported to exhibit antiproliferation activity against several cancer cultures in vitro (IC50 from 3 to 8 µM) and effectively suppress HCT-116-derived tumor growth in mice in vivo (50 mg/kg i.p.).
      Catalogue Number385570
      Brand Family Calbiochem®
      SynonymsHeat Shock Protein Inhibitor III, p-TEFb hsp70 Promoter Recruitment Inhibitor, N²-(1H-Indazol-5-yl)-N⁶-methyl-3-nitropyridine-2,6-diamine , HSF1 Inhibitor, KRIBB11, Hsp70 Induction Inhibitor II
      References
      ReferencesYoon, Y.J., et al. 2010. J. Biol. Chem. 286, 1737.
      Product Information
      FormOrange-yellow solid
      Hill FormulaC₁₃H₁₂N₆O₂
      Chemical formulaC₁₃H₁₂N₆O₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ200
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      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 -20°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

      Heat Shock Factor 1 Inhibitor, KRIBB11 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Heat Shock Factor 1 Inhibitor, KRIBB11 - Calbiochem Certificates of Analysis

      TitleLot Number
      385570

      References

      Reference overview
      Yoon, Y.J., et al. 2010. J. Biol. Chem. 286, 1737.
      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.

      Revision02-April-2012 JSW
      SynonymsHeat Shock Protein Inhibitor III, p-TEFb hsp70 Promoter Recruitment Inhibitor, N²-(1H-Indazol-5-yl)-N⁶-methyl-3-nitropyridine-2,6-diamine , HSF1 Inhibitor, KRIBB11, Hsp70 Induction Inhibitor II
      DescriptionA cell-permeable 2,6-diaminopyridine compound that interacts with HSF1 (heat shock factor 1) in a reversible manner and prevents HSF1 from recruiting p-TEFb (positive transcription elongation factor b) to the hsp70 promoter site (IC50 ≤3 µM in HCT-116 ChIP assays), a critical step for the p-TEFb CDK9 subunit-catalyzed pol II CTD (RNA polymerase II c-terminal domain) Ser-2 phosphorylation and transcription activation upon heat shock induction (IC50 <1, <3, <5, and <10 µM, respectively, against reporter, HSP47, HSP27, and HSP70 transcription in HCT-116 cultures). Reported to exhibit antiproliferation activity against several cancer cultures in vitro (IC50 ranges from 3 to 8 µM) and effectively suppress HCT-116-derived tumor growth in mice in vivo (by 47.4% on day 31; single i.p. dosage of 50 mg/kg on day 13 after cancer implantation). Does not affect TNF-α-induced NF-κB activity in HeLa or heat shock-induced HSF1 ser230 phosphorylation and promoter association in HCT-116 even at concentrations as high as 10 µM.
      FormOrange-yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₃H₁₂N₆O₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml; brown solution)
      Storage -20°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
      ReferencesYoon, Y.J., et al. 2010. J. Biol. Chem. 286, 1737.