385570

Heat Shock Factor 1 Inhibitor, KRIBB11

The Heat Shock Factor 1 Inhibitor, KRIBB11 controls the biological activity of Heat Shock Factor 1.

• Synonyme(s) : Heat Shock Factor 1 Inhibitor, KRIBB11, Hsp70 Induction Inhibitor II, N²-(1H-Indazol-5-yl)-N⁶-methyl-3-nitropyridine-2,6-diamine, HSF1 Inhibitor, KRIBB11, Heat Shock Protein Inhibitor III, p-TEFb hsp70 Promoter Recruitment Inhibitor
• Formule empirique (notation de Hill) : C₁₃H₁₂N₆O₂
• CAS Number: 342639-96-7
• Poids moléculaire : 284.27
• Numéro MDL: MFCD30182306
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 200
• Essai: ≥98% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: orange-yellow
• Solubilité: DMSO: 50 mg/mL, brown
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• Chaîne SMILES: CNC(C=C1)=NC(NC2=CC3=C(NN=C3)C=C2)=C1[N+]([O-])=O
• InChI: 1S/C13H12N6O2/c1-14-12-5-4-11(19(20)21)13(17-12)16-9-2-3-10-8(6-9)7-15-18-10/h2-7H,1H3,(H,15,18)(H2,14,16,17)
• Clé InChI: NDJJEQIMIJJCLL-UHFFFAOYSA-N

Description

Description générale

A 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.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

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

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable