WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555224
CAS#: 1196723-93-9
Description: HSF1A is an activator of Heat shock transcription factor 1 (HSF1).
MedKoo Cat#: 555224
Name: HSF1A
CAS#: 1196723-93-9
Chemical Formula: C21H19N3O2S2
Exact Mass: 409.0919
Molecular Weight: 409.522
Elemental Analysis: C, 61.59; H, 4.68; N, 10.26; O, 7.81; S, 15.66
Synonym: HSF1A;
IUPAC/Chemical Name: 4-Ethyl-N-[1-phenyl-3-(2-thienyl)-1H-pyrazol-5-yl]-benzenesulfonamide
InChi Key: KJTITGSAONQVPY-UHFFFAOYSA-N
InChi Code: 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
SMILES Code: O=S(C1=CC=C(CC)C=C1)(NC2=CC(C3=CC=CS3)=NN2C4=CC=CC=C4)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | HSF1A is a cell-permeable activator of heat shock transcription factor 1 (HSF1). |
| In vitro activity: | HSF1A blocked the intoxication process in a concentration-dependent manner. While initial effects were observed at 10 µM, HSF1A at 50 µM completely blocked TcdB-induced cytotoxicity. Reference: Proc Natl Acad Sci U S A. 2018 Sep 18;115(38):9580-9585. https://pubmed.ncbi.nlm.nih.gov/30181275/ |
| In vivo activity: | Collagen accumulation in the DOX-treated rat hearts was clearly increased, indicating that cardiac fibrosis had occurred, whereas HSF1A administration reduced the extent of cardiac fibrosis (Figure 7b). Reference: Cell Death Dis. 2016 Nov 3;7(11):e2455. https://pubmed.ncbi.nlm.nih.gov/27809308/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 116.0 | 283.26 |
The following data is based on the product molecular weight 409.522 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Steinemann M, Schlosser A, Jank T, Aktories K. The chaperonin TRiC/CCT is essential for the action of bacterial glycosylating protein toxins like Clostridium difficile toxins A and B. Proc Natl Acad Sci U S A. 2018 Sep 18;115(38):9580-9585. doi: 10.1073/pnas.1807658115. Epub 2018 Sep 4. PMID: 30181275; PMCID: PMC6156611. 2. Neef DW, Jaeger AM, Gomez-Pastor R, Willmund F, Frydman J, Thiele DJ. A direct regulatory interaction between chaperonin TRiC and stress-responsive transcription factor HSF1. Cell Rep. 2014 Nov 6;9(3):955-66. doi: 10.1016/j.celrep.2014.09.056. Epub 2014 Oct 30. PMID: 25437552; PMCID: PMC4488849. 3. Huang CY, Kuo WW, Lo JF, Ho TJ, Pai PY, Chiang SF, Chen PY, Tsai FJ, Tsai CH, Huang CY. Doxorubicin attenuates CHIP-guarded HSF1 nuclear translocation and protein stability to trigger IGF-IIR-dependent cardiomyocyte death. Cell Death Dis. 2016 Nov 3;7(11):e2455. doi: 10.1038/cddis.2016.356. PMID: 27809308; PMCID: PMC5260882. |
| In vitro protocol: | 1. Steinemann M, Schlosser A, Jank T, Aktories K. The chaperonin TRiC/CCT is essential for the action of bacterial glycosylating protein toxins like Clostridium difficile toxins A and B. Proc Natl Acad Sci U S A. 2018 Sep 18;115(38):9580-9585. doi: 10.1073/pnas.1807658115. Epub 2018 Sep 4. PMID: 30181275; PMCID: PMC6156611. 2. Neef DW, Jaeger AM, Gomez-Pastor R, Willmund F, Frydman J, Thiele DJ. A direct regulatory interaction between chaperonin TRiC and stress-responsive transcription factor HSF1. Cell Rep. 2014 Nov 6;9(3):955-66. doi: 10.1016/j.celrep.2014.09.056. Epub 2014 Oct 30. PMID: 25437552; PMCID: PMC4488849. |
| In vivo protocol: | 1. Huang CY, Kuo WW, Lo JF, Ho TJ, Pai PY, Chiang SF, Chen PY, Tsai FJ, Tsai CH, Huang CY. Doxorubicin attenuates CHIP-guarded HSF1 nuclear translocation and protein stability to trigger IGF-IIR-dependent cardiomyocyte death. Cell Death Dis. 2016 Nov 3;7(11):e2455. doi: 10.1038/cddis.2016.356. PMID: 27809308; PMCID: PMC5260882. |
1: Huang CY, Kuo WW, Lo JF, Ho TJ, Pai PY, Chiang SF, Chen PY, Tsai FJ, Tsai CH, Huang CY. Doxorubicin attenuates CHIP-guarded HSF1 nuclear translocation and protein stability to trigger IGF-IIR-dependent cardiomyocyte death. Cell Death Dis. 2016 Nov 3;7(11):e2455. doi: 10.1038/cddis.2016.356. PubMed PMID: 27809308; PubMed Central PMCID: PMC5260882.
2: Bocchini CE, Nahmod K, Katsonis P, Kim S, Kasembeli MM, Freeman A, Lichtarge O, Makedonas G, Tweardy DJ. Protein stabilization improves STAT3 function in autosomal dominant hyper-IgE syndrome. Blood. 2016 Dec 29;128(26):3061-3072. doi: 10.1182/blood-2016-02-702373. Epub 2016 Oct 31. PubMed PMID: 27799162; PubMed Central PMCID: PMC5201093.
3: Neef DW, Jaeger AM, Gomez-Pastor R, Willmund F, Frydman J, Thiele DJ. A direct regulatory interaction between chaperonin TRiC and stress-responsive transcription factor HSF1. Cell Rep. 2014 Nov 6;9(3):955-66. doi: 10.1016/j.celrep.2014.09.056. Epub 2014 Oct 30. PubMed PMID: 25437552; PubMed Central PMCID: PMC4488849.
4: Kawabe S, Yokoyama Y. Novel isoforms of heat shock transcription factor 1 are induced by hypoxia in the Pacific oyster Crassostrea gigas. J Exp Zool A Ecol Genet Physiol. 2011 Aug 1;315(7):394-407. doi: 10.1002/jez.685. Epub 2011 Mar 31. PubMed PMID: 21455948.
5: Neef DW, Turski ML, Thiele DJ. Modulation of heat shock transcription factor 1 as a therapeutic target for small molecule intervention in neurodegenerative disease. PLoS Biol. 2010 Jan 19;8(1):e1000291. doi: 10.1371/journal.pbio.1000291. PubMed PMID: 20098725; PubMed Central PMCID: PMC2808216.
6: Ojima N, Yamashita M. Cloning and characterization of two distinct isoforms of rainbow trout heat shock factor 1. Evidence for heterotrimer formation. Eur J Biochem. 2004 Feb;271(4):703-12. PubMed PMID: 14764086.
7: Airaksinen S, Jokilehto T, Råbergh CM, Nikinmaa M. Heat- and cold-inducible regulation of HSP70 expression in zebrafish ZF4 cells. Comp Biochem Physiol B Biochem Mol Biol. 2003 Oct;136(2):275-82. PubMed PMID: 14529753.
8: Murtha JM, Keller ET. Characterization of the heat shock response in mature zebrafish (Danio rerio). Exp Gerontol. 2003 Jun;38(6):683-91. PubMed PMID: 12814804.
