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Chemical Structure : CB-5083
CAS No.: 1542705-92-9
Catalog No.: PC-43263Not For Human Use, Lab Use Only.
CB-5083 is a potent, selective, orally bioavailable inhibitor of p97 AAA with IC50 of 11 nM, specifically targets D2 ATPase site of p97, shows 9.6, 128 and 158-fold less affinity for DNA-PK, mTOR and PIK3C3.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $98 | In stock | |
| 25 mg | $168 | In stock | |
| 50 mg | $268 | In stock | |
| 100 mg | $428 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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CB-5083 is a potent, selective, orally bioavailable inhibitor of p97 AAA with IC50 of 11 nM, specifically targets D2 ATPase site of p97, shows 9.6, 128 and 158-fold less affinity for DNA-PK, mTOR and PIK3C3.
CB-5083 causes accumulation of poly-ubiquitinated proteins, retention of ERAD substrates, and generation of irresolvable proteotoxic stress, leading to activation of the apoptotic arm of the unfolded protein response (UPR) in cancer cells.
CB-5083 inhibits A549 cell viability with IC50 of 0.67 uM, induces the UPR and apoptosis in xenograft tumor models.
| M.Wt | 413.4717 | |
| Formula | C24H23N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1H-Indole-4-carboxamide, 1-[7,8-dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl- |
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1. Anderson DJ, et al. Cancer Cell. 2015 Nov 9;28(5):653-665.
2. Zhou HJ, et al. J Med Chem. 2015 Dec 24;58(24):9480-97.
3. Le Moigne R, et al. Mol Cancer Ther. 2017 Nov;16(11):2375-2386.
4. Bastola P, et al. Mol Oncol. 2016 Dec;10(10):1559-1574.
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