An Hsf1 inhibitor (IC50 = 1.2 μM in a luciferase reporter assay); blocks heat shock-induced Hsp70

KRIBB11 – 5 mg

Brand:
Cayman
CAS:
342639-96-7
Storage:
-20
UN-No:
Non-Hazardous - /

KRIBB11 is an inhibitor of heat shock factor 1 (Hsf1) with an IC50 value of 1.2 μM in a luciferase reporter assay.{37149} It blocks heat shock-induced Hsp70, Hsp40, and Hsp27 mRNA expression and down-regulates protein expression of the Hsf1 target proteins Hsp70 and Hsp27 in HCT116 cells in a dose-dependent manner. KRIBB11 specifically binds to Hsf1 over other Hsf1-associated proteins, lacking activity at heat shock protein 90 (Hsp90), Hsf2, and Cdk9 in an in vitro pull-down assay. It inhibits growth of HCT116, Mia-PaCa-2, SW620, HT-29, A549, and MDA-MB-231 cancer cell lines (IC50s = 3-8 μM) via induction of cell cycle arrest at the G2/M phase and apoptosis. In vivo, administration of KRIBB11 decreases tumor growth in a mouse HCT116 xenograft model. KRIB11 administration also attenuates dengue virus progression and reduces mortality without affecting bodyweight in infected mice.{37150}  

 

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SKU: 9002528 - 5 mg Category:

Description

An Hsf1 inhibitor (IC50 = 1.2 μM in a luciferase reporter assay); blocks heat shock-induced Hsp70, Hsp40, and Hsp27 mRNA expression and down-regulates protein expression of the Hsf1 target proteins Hsp70 and Hsp27 in HCT116 cells in a dose-dependent manner; specifically binds to Hsf1 over other Hsf1-associated proteins, lacking activity at Hsp90, Hsf2, and Cdk9 in an in vitro pull-down assay; inhibits growth of cancer cell lines (IC50s = 3-8 μM) via induction of cell cycle arrest at the G2/M phase and apoptosis; decreases tumor growth in a mouse HCT116 xenograft model; attenuates dengue virus progression and reduces mortality in infected mice

Formal name: N2-1H-indazol-5-yl-N6-methyl-3-nitro-2,6-pyridinediamine

Synonyms: 

Molecular weight: 284.3

CAS: 342639-96-7

Purity: ≥95%

Formulation: A crystalline solid

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