SML3480

ULK-101

≥98% (HPLC)

• Synonym(s): (S)-N-(1-cyclopropyl-2,2,2-trifluoroethyl)-4-(6-(4-fluorophenyl)pyrazolo[1,5-a]pyrimidin-3-yl)thiophene-2-carboxamide, N-[(1S)-1-Cyclopropyl-2,2,2-trifluoroethyl]-4-[6-(4-fluorophenyl)pyrazolo[1,5-a]pyrimidin-3-yl]-2-thiophenecarboxamide, ULK 101, ULK101
• Empirical Formula (Hill Notation): C₂₂H₁₆F₄N₄OS
• CAS Number: 2443816-45-1
• Molecular Weight: 460.45
• MDL number: MFCD31813791
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C
• SMILES string: FC(F)(F)[C@H](C1CC1)NC(C2=CC(C3=C4N(N=C3)C=C(C5=CC=C(C=C5)F)C=N4)=CS2)=O

Description

Biochem/physiol Actions

ULK-101 is a potent and selective ULK1 inhibitor (ULK1/2 IC50 = 8.3/30 nM) that inhibits ULK1-dependent cellular Beclin 1 phosphorylation (pSer15 IC50 = 390 nM) with greater kinome selectivity (4 off-target hits using a 327-kinase panel) and potency than SBI-0206965 (IC50 = 38 nM/cell-free ULK1 kinase assay, 2.4 μM/cellular Beclion 1 pSer15). ULK-101 sensitizes cells to nutrient stress in U2OS (EC50 = 6.3 μM vs. 22.3 μM with full media) and in KRAS mutant lung cancer cultures (full media/nutrient withdrawal EC50 ratio >5) by suppressing autophagy induction and autophagic flux.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable