ULK-101

ULK-101 is an inhibitor of unc-51-like autophagy activating kinase 1 (ULK1) and ULK2 (IC50s = 8.3 and 30 nM, respectively). It is selective for ULK1 and ULK2 over a panel of 325 additional kinases at 10 µM but does inhibit serine/threonine kinase 17a (STK17A), also known as DRAK1, and MAP kinase-interacting serine/threonine protein kinase 2 (MNK2) (IC50s = 14 and 22 nM, respectively). ULK-101 inhibits nutrient starvation-induced phosphorylation of Beclin 1 in HEK293T cells (EC50 = 390 nM). It inhibits the formation of omegasomes positive for zinc finger FYVE-type containing 1 (ZFYVE1), also known as DFCP1, a marker of autophagy induction, in U2OS cells when used at a concentration of 5 µM. ULK-101 (1 and 2 µM) reduces the viability of nutrient-restricted H838, H727, H2030, and A549 lung cancer cells.Formal Name: N-[(1S)-1-cyclopropyl-2,2,2-trifluoroethyl]-4-[6-(4-fluorophenyl)pyrazolo[1,5-a]pyrimidin-3-yl]-2-thiophenecarboxamide. CAS Number: 2443816-45-1. Molecular Formula: C22H16F4N4OS. Formula Weight: 460.4. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble, DMSO: Soluble. SMILES: O=C(C1=CC(C(C=N2)=C3N2C=C(C(C=C4)=CC=C4F)C=N3)=CS1)N[C@@H](C5CC5)C(F)(F)F. InChi Code: InChI=1S/C22H16F4N4OS/c23-16-5-3-12(4-6-16)15-8-27-20-17(9-28-30(20)10-15)14-7-18(32-11-14)21(31)29-19(13-1-2-13)22(24,25)26/h3-11,13,19H,1-2H2,(H,29,31)/t19-/m0/s1. InChi Key: PFZRXJIYAFANHP-IBGZPJMESA-N.