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KGP94

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Chemical Structure| 1131456-28-4 同义名 : -
CAS号 : 1131456-28-4
货号 : A1678570
分子式 : C14H12BrN3OS
纯度 : 99%+
分子量 : 350.234
MDL号 : N/A
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(299.8 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 KGP94 is a selective cathepsin L inhibitor with an IC50 value of 189 nM[1].KGP94 inhibits migration and invasion of metastatic cancers and shows low cytotoxicity against a variety of human cell lines (GI50=26.9 µM)[2].At concentrations of 10 µM or 20 µM, acting for 24 hours, KGP94 reduces the expression of markers of macrophage M2 (arginase-1 and CD206) as well as cellular invasion by primary bone marrow-derived macrophages or Raw264.7[3].At a concentration of 25 μM for 24 hours of treatment, the effects of KGP94 on the invasive capacity of prostate and respiratory cancer cells were 53% and 88%, respectively, and the inhibition of CTSL activity secreted by PC-3ML and MDA-MB-231 was 94% and 92%, respectively[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.86mL

0.57mL

0.29mL

14.28mL

2.86mL

1.43mL

28.55mL

5.71mL

2.86mL
参考文献

[1]Parker EN, et al. Synthesis and biological evaluation of a water-soluble phosphate prodrug salt and structural analogues of KGP94, a lead inhibitor of cathepsin L. Bioorg Med Chem Lett. 2017 Mar 1. 27(5):1304-1310.

[2]Munikishore R, et al. An efficient and concise synthesis of a selective small molecule non-peptide inhibitor of cathepsin L: KGP94. Bioorg Chem. 2021 Nov. 116:105317.

[3]Dykes SS, et al. Cathepsin L secretion by host and neoplastic cells potentiates invasion. Oncotarget. 2019 Sep 17. 10(53):5560-5568.

[4]Sudhan DR, et al. Cathepsin L inhibition by the small molecule KGP94 suppresses tumor microenvironment enhanced metastasis associated cell functions of prostate and breast cancer cells. Clin Exp Metastasis. 2013 Oct. 30(7):891-902.

[5]Sudhan DR, et al. Cathepsin L inactivation leads to multimodal inhibition of prostate cancer cell dissemination in a preclinical bone metastasis model. Int J Cancer. 2016 Jun 1;138(11):2665-77.