Elesclomol Chemical Structure
NVP-AUY922 (VER-52296) is a highly potent HSP90 inhibitor to HSP90α and HSP90β with IC50 of 13 nM and 21 nM, respectively.
17-AAG (Geldanamycin) is a less toxic analogue of the geldanamycin which binds to Hsp90 and alters its function.
17-DMAG HCl (Alvespimycin) is a selective Hsp90 inhibitor with a GI50 of 53 nM.
Ganetespib is a unique triazolone-containing Hsp90 inhibitor with an IC50 of 4 nM for OSA 8 cells.
AT13387 is a selective potent small molecule heat shock protein 90 (Hsp90) inhibitor for A375, MV4-11, NCI-H1975 and SKBr3 cell lines with IC50 of 18 nM, 12 nM, 22 nM and 55 nM, respectively.
BIIB021 is an inhibitor of Hsp90(Ki=1.7nM).
MPC-3100 is a fully synthetic potent small-molecule Hsp90 inhibitor with an IC50 of 60 nM.
NVP-BEP800 is a novel, fully synthetic, oral Hsp90 inhibitor with an IC50 of 0.058 ± 0.006 μM.
SNX-2112 is a potent synthetic heat shock protein 90 inhibitor with an IC50 of 0.92 μM for K562 cells.
PF-04929113 (SNX-5422) is a potent and selective Hsp90 inhibitor with an IC50 of median 50 nM.
Elesclomol (STA-4783) is a small molecule that induces apoptosis via the mitochondrial apoptotic pathway in cancer cells by increasing oxidative stress, while having little or no effect on normal cells. It is a pro-apoptotic agent that demonstrates anti-tumor activity against a broad range of cancer cell types. It promotes apoptosis in Hs294T melanoma cells treated with 100 nmol/L for six hours by rapidly generating reactive oxygen species and inducing the transcription of Hsp70 and metallothionein.1 Stage III clinical trials to assess efficacy of elesclomol treatment in combination with paclitaxel2, 1 in patients with stage IV metastatic melanoma were suspended due to safety concerns.
| Molecular Weight (WM): | 400.5 |
|---|---|
| Formula: | C19H20N4O2S2 |
| CAS No.: | 488832-69-5 |
| Synonyms: |
STA-4783
|
| Dissolve in (25°C): | DMSO ≥80mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
A collection of 426 FDA approved drugs
A collection of 139 natural products
A collection of 40 chemotherapeutic agents
A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules
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