SML3480

ULK-101

Name: ULK-101
Brand: SIGMA

≥98% (HPLC), ULK1 inhibitor, powder

别名:

(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

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关于此项目

经验公式（希尔记法）:

C₂₂H₁₆F₄N₄OS

化学文摘社编号:

2443816-45-1

分子量:

460.45

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD31813791

主要文件

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产品名称

ULK-101, ≥98% (HPLC)

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

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

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Quality Level

100

Biochem/physiol Actions

Potent and selective ULK1 inhibitor that sensitizes cancer cells to nutrient stress by suppressing autophagy induction and autophagic flux.

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.