XST-14

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XST-14  纯度: 99.69%

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

XST-14 Chemical Structure

CAS No. : 2607143-50-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2750 In-stock
5 mg ￥2500 In-stock
10 mg ￥4500 In-stock
25 mg ￥8500 In-stock
50 mg ￥13500 In-stock
100 mg ￥19500 In-stock
200 mg   询价  
500 mg   询价  

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XST-14 相关产品

•相关化合物库:

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  • Targeted Diversity Library
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  • Anti-Colorectal Cancer Compound Library

生物活性

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].

IC50 & Target[1]

ULK1

26.6 nM (IC50)

体外研究
(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[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: HepG2 cells
Concentration: 20, 40, 60, 80 μM
Incubation Time: 24 hours
Result: Led a decrease in cell proliferation activity.

Apoptosis Analysis[1]

Cell Line: HepG2 and human primary cells
Concentration: 5 μM
Incubation Time: 24 hours
Result: Induced apoptosis in HepG2 and human primary HCC cells.

Cell Autophagy Assay[1]

Cell Line: CHO, HepG2 cells stably expressing GFP-LC3
Concentration: 5 μM
Incubation Time: 12 hours
Result: Strongly inhibited the conversion of LC3-I to LC3-II in CHO cells.
Dramatically decreased the number of GFP-LC3 puncta in HepG2 cells.
Decreased autophagosome formation and blocked autophagosome/lysosome fusion in HepG2 cells.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 5 μM
Incubation Time: 12 hours
Result: Inhibited the Ser249 phosphorylation of PIK3C3 and Ser15 phosphorylation of BECN1.

体内研究
(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[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice bearing HepG2 tumor xenografts[1]
Dosage: 15, 30 mg/kg
Administration: IP; daily; for 4 consecutive weeks
Result: Displayed anti-HCC efficacies, resulting in decreased tumor weights and suppressed tumor growth of HCC cells in nude mice.
Animal Model: Sprague-Dawley rat[1]
Dosage: 2 mg/kg for IV; 10 mg/kg for IP (Pharmacokinetic Analysis)
Administration: IV or IP
Result: Had a T1/2 of 2.31 hours, a CL of 26.28 mL/min•kg, and and an AUC of 1269 hr•ng/mL for IV.
Had a T1/2 of 2.69 hours, a Cmax of 2033 ng/mL, and an AUC of 5979 hr•ng/mL for IP.

分子量

291.34

Formula

C16H21NO4
CAS 号

2607143-50-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (858.10 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4324 mL 17.1621 mL 34.3242 mL
5 mM 0.6865 mL 3.4324 mL 6.8648 mL
10 mM 0.3432 mL 1.7162 mL 3.4324 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.14 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.14 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [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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