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PubMed PMID: 24804890
Smiles: O=C1CC2=CC(CCN3CCN(CC3)C3=NSC4=CC=CC=C43)=C(Cl)C=C2N1
PNRI-299 has no effect on NF-κB transcription (up to 200 uM) or thioredoxin (up to 200 uM)
Chronic treatment with novel GPR40 agonists improve whole-body glucose metabolism based on the glucose-dependent insulin secretion
In cell cultures as well as in animal models
CB-6644 - CAS# 2316817-88-4 BI-98782 PubMed PMID: 24804890CB 6644 is a novel allosteric selective inhibitor of the ruvbl1 2 complex with anti cancer activity. CB 6644 blocks the ATPase activity of RUVBL1 2 with an IC50 of 15 nM. CB 6644 interacts specifically with RUVBL1 2 in cancer cells, leading to cell death. Importantly, drug acquired resistant cell clones have amino acid mutations in either RUVBL1 or RUVBL2, suggesting that cell killing is an on target consequence of RUVBL1 2 engagement. In xenograft
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