Chemical Structure : RUVBL1/RUVBL2 inhibitor Compound B
CAS No.:
1807337-58-1
RUVBL1/RUVBL2 inhibitor Compound B
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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536.03
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Formula
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C28H30ClN5O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(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
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References
1. Yenerall P, et al. Cell Chem Biol. 2020 Jan 16;27(1):105-121.e14.
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