HSF1 Activator HSF1A

A cell-permeable pyrazolylsulfonamide compound that activates heat shock factor 1 (HSF1) and protects mammalian cells against stress-induced apoptosis. Offers protection against ER stress-induced apoptosis as indicated by blunting of caspase-3 activity in treated cells. Shown to activate human HSF1 function in yeast cells. Promotes the nuclear localization and phosphorylation of HSF1 (within 2 h of treatment). Activates Hsp25 and Hsp70 expression in wild-type mouse embryonic fibroblasts (~ 30 µM) and Hsp70 in HeLa cells. Shown to directly and reversibly interact with cytosolic chaperonin TRiC/CCT subunit (K_d = 613 nM for HSF1A-FITC and Tcp1), involving the hinge 2 region, and destabilize TRiC/CCT-HSF1 association. However, it does not perturb ATP hydrolysis. Reduces protein misfolding and cell death in PolyQ-expressing neuronal precursor cells and protects against cytotoxicity in Drosophila melanogaster model of PolyQ-mediated neurodegeneration.

HSF1 Activator, HSF1A, CAS 1196723-93-9, is a cell-permeable activator of HSF1 that protects mammalian cells against stress-induced apoptosis. Protects cells from polyQ cytotoxicity.

Cell permeable: yes

Primary Target
HSF1

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Neef, D.W., et al. 2014. Cell Reports.9, 955.
Neef, D.W., et al. 2010. PLoS Biology.8, e1000291.

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

Toxicity: Standard Handling (A)