1884220-36-3 Usage
Description
ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation. It is activated by phosphorylation by AMPK and, in turn, phosphorylates and inhibits AMPK. SBI-0206965 is an inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM). It is selective for ULK1 and ULK2 over a panel of 456 additional kinases, showing activity against a few kinases in vitro but not in cells. SBI-0206965 suppresses autophagy induced by mTOR inhibition via AZD 8055 . It also blocks ULK1-dependent cell survival following nutrient deprivation.
Uses
SBI-0206965 is an inhibitor of ULK1. It also blocks ULK1-dependent cell survival following nutrient deprivation. ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation.
Biochem/physiol Actions
Since most of the tumor cells survive on autophagy mechanism, inhibition of autophagy inducers Unc-51 (serine/threonine-protein kinase)-like autophagy activating kinase (ULK1 and ULK2) might be useful in cancer therapy.
References
1) Egan?et al. (2015), Small Molecules Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates; Mol. Cell, 59?285
Check Digit Verification of cas no
The CAS Registry Mumber 1884220-36-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,8,8,4,2,2 and 0 respectively; the second part has 2 digits, 3 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1884220-36:
(9*1)+(8*8)+(7*8)+(6*4)+(5*2)+(4*2)+(3*0)+(2*3)+(1*6)=183
183 % 10 = 3
So 1884220-36-3 is a valid CAS Registry Number.
1884220-36-3Relevant articles and documents
NOVEL ULK1 INHIBITORS AND METHODS USING SAME
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Page/Page column 176; 175, (2016/03/22)
In certain aspects, the invention provides a method for treating a disease or condition in a subject, the method comprising co-administering to a subject in need thereof a therapeutically effective amount of at least one ULK1-inhibiting pyrimidine, and a therapeutically effective amount of an mTOR inhibitor.
