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385570 Heat Shock Factor 1 Inhibitor, KRIBB11 - Calbiochem

385570
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₃H₁₂N₆O₂

Products

Catalogue NumberPackaging Qty/Pack
385570-10MG Glass bottle 10 mg
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®
SynonymsHsp70 Induction Inhibitor II, Heat 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
References
ReferencesYoon, Y.J., et al. 2010. J. Biol. Chem. 286, 1737.
Product Information
CAS number342639-96-7
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
SynonymsHsp70 Induction Inhibitor II, Heat 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
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
CAS number342639-96-7
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.