Formulation: A solid
Formal Name: N-[(1S)-1-cyclopropyl-2,2,2-trifluoroethyl]-4-[6-(4-fluorophenyl)pyrazolo[1,5-a]pyrimidin-3-yl]-2-thiophenecarboxamide
Purity: ≥95%
Formula Markup: C22H16F4N4OS
Formula Weight: 460,4
Shelf life (days): 1460
CAS Number: 2443816-45-1
Notes: ULK-101 is an inhibitor of unc-51-like autophagy activating kinase 1 (ULK1) and ULK2 (IC50s = 8.3 and 30 nM, respectively).{67648} 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.
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