CB-5083 |CAS:1542705-92-9 Probechem Biochemicals

Chemical Structure : CB-5083

CAS No.: 1542705-92-9

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CB-5083 (CB5083, CB 5083)

货号: 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.

规格	价格	库存
10 mg	￥980	In stock
25 mg	￥1680	In stock
50 mg	￥2680	In stock
100 mg	￥4280	In stock
200 mg		Get quote
1 g		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	413.4717
分子式	C24H23N5O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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-

参考文献

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.

CB-5083 (CB5083, CB 5083)

生物&药学活性

物理化学性质&存储条件

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CB-5083 (CB5083, CB 5083)

生物&药学活性

物理化学性质&存储条件

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