RGNCY-0090 (ULK-101 Autophagy inhibitor)

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ULK-101 is a selective and potent inhibitor of autophagy.  ULK-101 suppresses autophagy induction and autophagic flux in response to a variety of stimuli.  ULK-101 inhibition is able to sensitize KRAS mutant lung cancer cells to nutrient stress.  ULK-101 is a promising target for autophagy inhibition due to its central role in in pathway activation, druggability and selectivity for autophagy.  ULK1 inhibition IC50 = 8.3nM.

SMILE:  FC1=CC=C(C(C=N2)=CN3C2=C(C4=CSC(C(N[C@@H](C5CC5)C(F)(F)F)=O)=C4)C=N3)C=C1

Systematic Name:   (S)-N-(1-cyclopropyl-2,2,2-trifluoroethyl)-4-(6-(4-fluorophenyl)pyrazolo[1,5-a]pyrimidin-3-yl)thiophene-2-carboxamide

Molecular Weight:  460.45

Formula:  C22H16F4N4OS

PMID:  30292171