貨號	規格	價格	上海	北京	武漢	南京
S23287-1mg	≥98%	￥940.00 S23287-1mg ￥940.00 2-3天	0 貨期：2-3天	-	-	-
S23287-5mg	≥98%	￥2350.00 S23287-5mg ￥2350.00 2-3天	0 貨期：2-3天	-	-	-
S23287-10mg	≥98%	￥3500.00 S23287-10mg ￥3500.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

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

產品描述：

靶點：

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：

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 抑制轉移癌的運動性和侵襲性，對人類細胞的毒性低 (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

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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