5.33761

HSF1 Activator HSF1A

• Synonym(s): HSF1 Activator HSF1A, Heat Shock Factor 1 Activator, HSF1A
• Empirical Formula (Hill Notation): C₂₁H₁₉N₃O₂S₂
• CAS Number: 1196723-93-9
• Molecular Weight: 409.52
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C
• InChI: 1S/C21H19N3O2S2/c1-2-16-10-12-18(13-11-16)28(25,26)23-21-15-19(20-9-6-14-27-20)22-24(21)17-7-4-3-5-8-17/h3-15,23H,2H2,1H3
• InChI key: KJTITGSAONQVPY-UHFFFAOYSA-N

Description

General description

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.

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.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
HSF1

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable