Molecular structure of VER-49009, CAS Number: 940289-57-6
VER-49009 (CAS 940289-57-6)
Alternate Names:
3-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)-1H-pyrazole-5-carboxamide
Application:
VER-49009 is an inhibitor of Hsp90
CAS Number:
940289-57-6
Molecular Weight:
387.8
Molecular Formula:
C19H18ClN3O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
The heat shock proteins (Hsps) act as molecular chaperones. Hsp90 is an abundant protein with roles in protein folding, cell signaling, and cancer. VER-49009 is a pyrazole compound that inhibits Hsp90 with an IC50 value of 47 nM. It produces a cellular antiproliferative GI50 value of 685 nM when tested against a human cancer cell line panel. Consistent with inhibition of Hsp90, VER-49009 induces the expression of Hsp27 and Hsp72 while reducing the client proteins C-RAF, B-RAF, survivin, and PRMT5, causing cell cycle arrest and apoptosis.
VER-49009 (CAS 940289-57-6) References
- Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. | Dymock, BW., et al. 2005. J Med Chem. 48: 4212-5. PMID: 15974572
- 4-Amino derivatives of the Hsp90 inhibitor CCT018159. | Barril, X., et al. 2006. Bioorg Med Chem Lett. 16: 2543-8. PMID: 16480864
- Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues. | Sharp, SY., et al. 2007. Mol Cancer Ther. 6: 1198-211. PMID: 17431102
- Silencing the cochaperone CDC37 destabilizes kinase clients and sensitizes cancer cells to HSP90 inhibitors. | Smith, JR., et al. 2009. Oncogene. 28: 157-69. PMID: 18931700
- Acquired resistance to 17-allylamino-17-demethoxygeldanamycin (17-AAG, tanespimycin) in glioblastoma cells. | Gaspar, N., et al. 2009. Cancer Res. 69: 1966-75. PMID: 19244114
- Inhibition of hepatic stellate cell proliferation by heat shock protein 90 inhibitors in vitro. | Sun, X., et al. 2009. Mol Cell Biochem. 330: 181-5. PMID: 19412730
- Discovery of hybrid Hsp90 inhibitors and their anti-neoplastic effects against gefitinib-resistant non-small cell lung cancer (NSCLC). | Jeong, CH., et al. 2014. Bioorg Med Chem Lett. 24: 224-7. PMID: 24345447
- A cell-based high-content screen identifies isocotoin as a small molecule inhibitor of the meiosis-specific MEIOB-SPATA22 complex†. | Xu, Y., et al. 2020. Biol Reprod. 103: 333-342. PMID: 32463099
- Evolution of kinase polypharmacology across HSP90 drug discovery. | Antolin, AA., et al. 2021. Cell Chem Biol. 28: 1433-1445.e3. PMID: 34077750
- ROS/MMP-9 mediated CS degradation in BMSC inhibits citric acid metabolism participating in the dual regulation of bone remodelling. | Da, W., et al. 2024. Cell Death Discov. 10: 77. PMID: 38355572
Inhibitor of:
HSP 90.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
VER-49009, 500 µg | sc-357409 | 500 µg | $123.00 | |||
VER-49009, 1 mg | sc-357409A | 1 mg | $235.00 | |||
VER-49009, 5 mg | sc-357409B | 5 mg | $992.00 | |||
VER-49009, 10 mg | sc-357409C | 10 mg | $1725.00 |