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RUVBL1/RUVBL2 inhibitor Compound B

Chemical Structure : RUVBL1/RUVBL2 inhibitor Compound B

CAS No.: 1807337-58-1

RUVBL1/RUVBL2 inhibitor Compound B

货号: PC-25731Not For Human Use, Lab Use Only.

RUVBL1/RUVBL2 inhibitor Compound B is a potent, specific and orally bioavailable RUVBL1/2 ATPase (pontin/TIP49 and reptin/TIP48) inhibitor with IC50 of 59 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

RUVBL1/RUVBL2 inhibitor Compound B is a potent, specific and orally bioavailable RUVBL1/2 ATPase (pontin/TIP49 and reptin/TIP48) inhibitor with IC50 of 59 nM.
Compound B (100 nM) depleted PIKK-family members DNA-PKCS (PRKDC), ATM, and ATR in H2009 cells, all of which require RUVBL1/2 ATPase activity for stability.
Compound B treatment reduced the levels of ATM, ATR, and DNA-PKCS in mice bearing subcutaneous NSCLC xenografts.
Compound B kills NSCLC due to the inhibition of RUVBL1/2.
Compound B inhibits PAQosome maturation.
Compound B radiosensitizes NSCLC, but not normal cells.

物理化学性质&存储条件

分子量 536.03
分子式 C28H30ClN5O4
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

(1R,3S)-3-(5-(5-chloro-2-ethoxyphenyl)-1,3,4-oxadiazol-2-yl)-N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)cyclohexane-1-carboxamide

参考文献

1. Yenerall P, et al. Cell Chem Biol. 2020 Jan 16;27(1):105-121.e14.

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