945377-65-1
Chemical Structure
ULK-100
- CAS No.: 945377-65-1
- Formula:C29H32F3N5O2S
- Molecular Weight:571.66
IUPAC Name: (S)-4-(6-(4-(2-(piperidin-1-yl)ethoxy)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)-N-(1,1,1-trifluoro-3-methylbutan-2-yl)thiophene-2-carboxamide
InChIKey: KYPQUQARPVLCEI-SANMLTNESA-N
SMILES: O=C(C1=CC(C2=C3N=CC(C4=CC=C(OCCN5CCCCC5)C=C4)=CN3N=C2)=CS1)N[C@@H](C(C)C)C(F)(F)F
Biological Activity: ULK-100 is a potent ULK1/ULK2 inhibitor, with IC50 values of 1.6 nM and 2.6 nM against human ULK1 and ULK2, respectively. ULK-100 reduces ULK1-mediated phosphorylation of Beclin 1 at Ser15, inhibits autophagy by targeting the ULK1 pathway, and also suppresses autophagy in tumor cells. ULK-100 enhances the sensitivity of tumor cells to nutrient deprivation. ULK-100 can be used in research on autophagy initiation and cancer[1][2].
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ULK-100 | ULK-100 is a potent ULK1/ULK2 inhibitor, with IC50 values of 1.6 nM and 2.6 nM against human ULK1 and ULK2, respectively. ULK-100 reduces ULK1-mediated phosphorylation of Beclin 1 at Ser15, inhibits autophagy by targeting the ULK1 pathway, and also suppresses autophagy in tumor cells. ULK-100 enhances the sensitivity of tumor cells to nutrient deprivation. ULK-100 can be used in research on autophagy initiation and cancer. | |||||||||||||||||||||
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References
- [1]. Martin KR, et al. A Potent and Selective ULK1 Inhibitor Suppresses Autophagy and Sensitizes Cancer Cells to Nutrient Stress. iScience. 2018 Oct 26;8:74-84. [Content Brief]
- [2]. Liu L, et al. A Review of ULK1-Mediated Autophagy in Drug Resistance of Cancer. Cancers. 2020 Feb 04;12(2):352. [Content Brief]
