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XST-14

CAS No. : 2607143-50-8

MCE 站：XST-14

产品活性：XST-14 是一种有效的，竞争性强且高度选择性的 ULK1 抑制剂，IC₅₀ 为 26.6 nM。XST-14 通过减少 ULK1 下游底物的磷酸化来诱导自噬抑制。XST-14 诱导肝细胞癌 (HCC) 细胞凋亡，并具有抗肿瘤作用。

研究领域：Autophagy  |  MAPK/ERK Pathway  |  TGF-beta/Smad  |  Protein Tyrosine Kinase/RTK  |  Neuronal Signaling

作用靶点：ULK  |  p38 MAPK  |  TGF-β Receptor  |  ALK  |  CaMK

In Vitro: 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.
XST-14 (20-80 μM; for 24 h) leads a decrease in cell proliferation activity.
XST-14 (5 μM; for 24 h) induces apoptosis in HepG2 and human primary HCC cells.
XST-14 (5 μM; for 12 h) strongly inhibits the conversion of LC3-I to LC3-II in CHO cells stably expressing GFP-LC3.
XST-14 (5 μM; for 12 h) inhibits the Ser249 phosphorylation of PIK3C3 and Ser15 phosphorylation of BECN1.

In Vivo: 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.
XST-14 (2 mg/kg for IV; 10 mg/kg for IP) has a T_1/2 of 2.31 hours for IV and a T_1/2 of 2.69 hours for IP.

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