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XST-14

CAS No. : 2607143-50-8

MCE 国际站：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.

相关产品：Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | MAPK Compound Library | Neuronal Signaling Compound Library | Protein Tyrosine Kinase Compound Library | TGF-beta/Smad Compound Library | Anti-Cancer Compound Library | Autophagy Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Pyroptosis Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | SB 203580 | SB-431542 | Dorsomorphin | SB 202190 | A 83-01 | KN-93 | LDN193189 | Doramapimod | RepSox | SB 525334 | STO-609 | DMH-1 | MRT67307 | SB-505124 | MRT68921 dihydrochloride | ULK-101 | Hesperetin | PD 169316 | K-252a | Neflamapimod | BMP signaling agonist sb4 | TAK⁻⁷15 | GW788388 | ITD-1 | KN-62

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