KGP94 98%

KGP94

源叶(MedMol)
S23287
1131456-28-4
C14H12BrN3OS
350.23
品牌 货号 产品规格 价格(RMB) 库存(上海) 北京 武汉 南京 购买数量
源叶(MedMol) S23287-1mg 98% ¥940.00元 预计交期:2-3天 - - -
源叶(MedMol) S23287-5mg 98% ¥2350.00元 预计交期:2-3天 - - -
源叶(MedMol) S23287-10mg 98% ¥3500.00元 预计交期:2-3天 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

KGP94 is a selective inhibitor of cathepsin L with an IC50 of 189 nM. KGP94 inhibits migration and invasion of metastatic carcinoma and shows low cytotoxicity (GI50=26.9 µM) against various human cell lines
产品描述: KGP94 is a selective inhibitor of cathepsin L with an IC50 of 189 nM. KGP94 inhibits migration and invasion of metastatic carcinoma and shows low cytotoxicity (GI50=26.9 µM) against various human cell lines
靶点: 189 nM (cathepsin L);CysteineProtease
体外研究: KGP94 (10 or 20 μM, 24 h) reduces expression of M2 (macrophage) markers (Arginase-1 and CD206) and cells invasion of primary bone marrow-derived macrophages or Raw264.7.

KGP94 (25 μM, 24 h) impairs the incasive capacities of both prostate and breat cancer cells by 53% and 88%, respectively.

KGP94 (25 μM, 24 h) suppresses secreted CTSL activity by 94% and 92% in PC-3ML and MDA-MB-231, repsectively.
体内研究: KGP94 (i.p.; 20 mg/kg; once daily for 3 days) exhibits anti-metastatic and anti-bone resorptive efficacy in a prostate cancer bone metastasis model. Animal Model: NCR nu/nu male mice Dosage: 20 mg/kg Administration: Intraperitoneal injection; once daily for 3 days Result: Reduced 65% in metastatic tumor burden and 58% in tumor angiogenesis, improved survival of bone metastases bearing mice.
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.
溶解性: Soluble  in  DMSO
保存条件: -20℃
备注: KGP94 是一种特异的 cathepsin L 抑制剂,IC50为 189 nM。KGP94 抑制转移癌的运动性和侵袭性,对人类细胞的毒性低 (GI50=26.9µM)。
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.855 ml 14.276 ml 28.553 ml
5 mM 0.571 ml 2.855 ml 5.711 ml
10 mM 0.286 ml 1.428 ml 2.855 ml
50 mM 0.057 ml 0.286 ml 0.571 ml
注意: 部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。

参考文献

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