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CB-5083

Chemical Structure : CB-5083

CAS No.: 1542705-92-9

CB-5083 (CB5083, CB 5083)

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 413.4717
Formula C24H23N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-Indole-4-carboxamide, 1-[7,8-dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-

References

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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