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KGP94 {[allProObj[0].p_purity_real_show]}

货号:A1678570 Ambeed 开学季,买赠积分,赢豪礼

KGP94是一种特异性 cathepsin L 抑制剂,IC50 值为 189 nM,能抑制癌细胞的迁移和侵袭,同时对正常人类细胞的毒性较低 (GI50=26.9µM),适用于癌症转移研究。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
KGP94 化学结构 CAS号:1131456-28-4
KGP94 化学结构
CAS号:1131456-28-4
KGP94 3D分子结构
CAS号:1131456-28-4
KGP94 化学结构 CAS号:1131456-28-4
KGP94 3D分子结构 CAS号:1131456-28-4
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KGP94 纯度/质量文件 产品仅供科研

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KGP94 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].

KGP94 动物研究

Animal study At a dose of 20 mg/kg, injected intraperitoneally once a day for 3 days, KGP94 showed anti-metastatic and anti-bone resorption efficacy in a bone metastasis model of prostate cancer. Metastatic tumour burden was reduced by 65%, tumour angiogenesis was reduced by 58%, and survival was improved in mice with bone metastases[5].

KGP94 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.

KGP94 实验方案

计算器
存储液制备 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

KGP94 技术信息

CAS号1131456-28-4
分子式C14H12BrN3OS
分子量 350.234
别名
运输蓝冰
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
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