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。

XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC 50 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.

Solid

CaMK II ULK1 26.6 nM (IC50)

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.
has not independently confirmed the accuracy of these methods.

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 250 mg/mL (858.10 mM; Need ultrasonic)配制储备液