XST-14 is a potent, highly selective inhibitor for Unc-51-Like Kinase 1 (ULK1) with IC50 of 13.6 nM and SPR KD of 30.75 nM. XST-14 (5 μM) only inhibits 6 out of 403 kinases by at least 75%, including ULK1 (MAP2K1/MEK1, MAPK14/p38 alpha, TGFBR2, ACVR1/ALK2, ULK2 and CAMK2A IC50 of 721.8, 283.9, 809.3, 183.8, 70.9, and 66.3 nM, respectively). XST-14 inhibits autophagy by reducing ULK1 kinase activity, strongly inhibits the conversion of LC3-I to LC3-II. XST-14 inhibited the Ser249 phosphorylation of PIK3C3 and Ser15 phosphorylation of BECN1. XST-14 acts synergistically with sorafenib to suppress HCC in vitro. XST-14 acts synergistically with sorafenib to suppress HCC tumor growth.
Physicochemical Properties
M.Wt
291.35
Formula
C16H21NO4
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
Methyl 4,6-diisopropoxy-1H-indole-2-carboxylate
References
1. Xue ST, et al. Autophagy. 2020 Oct;16(10):1823-1837.
