Synonym
SEW84; SEW 84; SEW-84;
IUPAC/Chemical Name
2-(1-(4-fluorophenyl)-1H-pyrrole-2-carbonyl)-N-(3-(trifluoromethyl)phenyl)hydrazine-1-carbothioamide
InChi Key
QEJONNSHVNSZBJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H14F4N4OS/c20-13-6-8-15(9-7-13)27-10-2-5-16(27)17(28)25-26-18(29)24-14-4-1-3-12(11-14)19(21,22)23/h1-11H,(H,25,28)(H2,24,26,29)
SMILES Code
S=C(NNC(C1=CC=CN1C2=CC=C(F)C=C2)=O)NC3=CC=CC(C(F)(F)F)=C3
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
To be determined
Shelf Life
>3 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:
SEW84 is a potent and selective inhibitor of the Aha1-stimulated Hsp90 ATPase activity without inhibition of basal Hsp90 ATPase. It binds to the C-terminal domain of Aha1 and weakens the Hsp90-Aha1 interaction. SEW84 inhibits Aha1-dependent Hsp90 chaperoning activities including refolding of denatured firefly luciferase (in vitro) and in vivo transcriptional activity of the glucocorticoid receptor and AR androgen receptor in prostate cancer cell-based models.
In vitro activity:
SEW84 blocks Aha1-dependent Hsp90 chaperoning activities, including the in vitro refolding of firefly luciferase and the transcriptional activity of the androgen receptor in cell-based models of prostate cancer.
Reference: Cell Chem Biol. 2020 Mar 19;27(3):292-305.e6. https://pubmed.ncbi.nlm.nih.gov/32017918/
In vivo activity:
SEW84 blocks Aha1-dependent Hsp90 chaperoning activities, including the in vivo refolding of firefly luciferase, and promotes the clearance of phosphorylated tau in cellular and tissue models of neurodegenerative tauopathy.
Reference: Cell Chem Biol. 2020 Mar 19;27(3):292-305.e6. https://pubmed.ncbi.nlm.nih.gov/32017918/
Preparing Stock Solutions
The following data is based on the
product
molecular weight
422.40
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. Singh JK, Hutt DM, Tait B, Guy NC, Sivils JC, Ortiz NR, Payan AN, Komaragiri SK, Owens JJ, Culbertson D, Blair LJ, Dickey C, Kuo SY, Finley D, Dyson HJ, Cox MB, Chaudhary J, Gestwicki JE, Balch WE. Management of Hsp90-Dependent Protein Folding by Small Molecules Targeting the Aha1 Co-Chaperone. Cell Chem Biol. 2020 Mar 19;27(3):292-305.e6. doi: 10.1016/j.chembiol.2020.01.008. Epub 2020 Feb 3. PMID: 32017918; PMCID: PMC7144688.
In vitro protocol:
1. Singh JK, Hutt DM, Tait B, Guy NC, Sivils JC, Ortiz NR, Payan AN, Komaragiri SK, Owens JJ, Culbertson D, Blair LJ, Dickey C, Kuo SY, Finley D, Dyson HJ, Cox MB, Chaudhary J, Gestwicki JE, Balch WE. Management of Hsp90-Dependent Protein Folding by Small Molecules Targeting the Aha1 Co-Chaperone. Cell Chem Biol. 2020 Mar 19;27(3):292-305.e6. doi: 10.1016/j.chembiol.2020.01.008. Epub 2020 Feb 3. PMID: 32017918; PMCID: PMC7144688.
In vivo protocol:
1. Singh JK, Hutt DM, Tait B, Guy NC, Sivils JC, Ortiz NR, Payan AN, Komaragiri SK, Owens JJ, Culbertson D, Blair LJ, Dickey C, Kuo SY, Finley D, Dyson HJ, Cox MB, Chaudhary J, Gestwicki JE, Balch WE. Management of Hsp90-Dependent Protein Folding by Small Molecules Targeting the Aha1 Co-Chaperone. Cell Chem Biol. 2020 Mar 19;27(3):292-305.e6. doi: 10.1016/j.chembiol.2020.01.008. Epub 2020 Feb 3. PMID: 32017918; PMCID: PMC7144688.
Singh JK, Hutt DM, Tait B, Guy NC, Sivils JC, Ortiz NR, Payan AN, Komaragiri SK, Owens JJ, Culbertson D, Blair LJ, Dickey C, Kuo SY, Finley D, Dyson HJ, Cox MB, Chaudhary J, Gestwicki JE, Balch WE. Management of Hsp90-Dependent Protein Folding by Small Molecules Targeting the Aha1 Co-Chaperone. Cell Chem Biol. 2020 Mar 19;27(3):292-305.e6. doi: 10.1016/j.chembiol.2020.01.008. Epub 2020 Feb 3. PMID: 32017918; PMCID: PMC7144688.
