產品屬性：
產品名稱 | XST-14 |
規格 | 10mM*1 mL in DMSO、5 mg、10 mg、25 mg、50 mg、100 mg |
貨號 | EY-01Y14093 |
Cas No.: 2607143-50-8
別名: N/A
化學名: N/A
分子式: C16H21NO4
分子量: 291.34
溶解度: DMSO : 250 mg/mL (858.10 mM; Need ultrasonic)
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
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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