XST-14 |
| Catalog No.GC62146 |
XST-14는 IC50이 26.6nM인 강력하고 경쟁적이며 고도로 선택적인 ULK1 억제제입니다. XST-14는 ULK1 다운스트림 기질의 인산화를 감소시켜 자가포식 억제를 유도합니다. XST-14는 간세포 암종(HCC) 세포에서 세포자멸사를 유도하고 항종양 효과가 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2607143-50-8
Sample solution is provided at 25 µL, 10mM.
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XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects[1].
XST-14 inhibits ULK1 (IC50=13.6 nM), MAP2K1/MEK1 (IC50=721.8 nM), MAPK14/p38 alpha (IC50=283.9 nM), TGFBR2 (IC50=809.3 nM), ACVR1/ALK2 (IC50=183.8 nM), ULK2 (IC50=70.9 nM) and CAMK2A (IC50=66.3 nM) by the 10-point titration results from SelectScreen Kinase Profiling Services[1]. XST-14 (20-80 μM; for 24 h) leads a decrease in cell proliferation activity[1]. XST-14 (5 μM; for 24 h) induces apoptosis in HepG2 and human primary HCC cells[1]. XST-14 (5 μM; for 12 h) strongly inhibits the conversion of LC3-I to LC3-II in CHO cells stably expressing GFP-LC3[1]. XST-14 (5 μM; for 12 h) inhibits the Ser249 phosphorylation of PIK3C3 and Ser15 phosphorylation of BECN1[1].
XST-14 (15, 30 mg/kg/day; IP; for 4 consecutive weeks) displays anti-HCC efficacies, resulting in decreased tumor weights and suppressed tumor growth of HCC cells in nude mice[1]. XST-14 (2 mg/kg for IV; 10 mg/kg for IP) has a T1/2 of 2.31 hours for IV and a T1/2 of 2.69 hours for IP[1].
[1]. Si-Tu Xue, et al. The role of the key autophagy kinase ULK1 in hepatocellular carcinoma and its validation as a treatment target . Autophagy. 2020 Oct;16(10):1823-1837.
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