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KGP94 98%

KGP94

源葉(MedMol)
S23287
1131456-28-4
C14H12BrN3OS
350.23
品牌 貨號 產(chǎn)品規(guī)格 價格(RMB) 庫存（上海） 北京 武漢 南京 購買數(shù)量
源葉(MedMol) S23287-1mg 98% ￥940.00元 預(yù)計(jì)交期：2-3天 - - -
源葉(MedMol) S23287-5mg 98% ￥2350.00元 預(yù)計(jì)交期：2-3天 - - -
源葉(MedMol) S23287-10mg 98% ￥3500.00元 預(yù)計(jì)交期：2-3天 - - -
產(chǎn)品介紹 參考文獻(xiàn) 質(zhì)檢證書(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

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
產(chǎn)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
靶點(diǎn)： 189 nM (cathepsin L);CysteineProtease
體外研究： 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.
體內(nèi)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.
參考文獻(xiàn)： 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
保存條件： -20℃
備注： KGP94 是一種特異的 cathepsin L 抑制劑，IC50為 189 nM。KGP94 抑制轉(zhuǎn)移癌的運(yùn)動性和侵襲性，對人類細(xì)胞的毒性低 (GI50=26.9μM)。
配置溶液濃度參考：
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
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參考文獻(xiàn)

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