| Company Name: |
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
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| Tel: |
17702719238 17702719238 |
| Email: |
sales@sun-shinechem.com |
| Products Intro: |
Product Name:KGP-94
CAS:1131456-28-4
Purity:98% HPLC Package:50.0mg;100.0mg; 200.0mg;500mg;1g;5g; 10g
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| Company Name: |
Tianjin Kailiqi Biotechnology Co., Ltd.
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| Tel: |
15076683720 |
| Email: |
klq@cw-bio.com |
| Products Intro: |
Product Name:KGP-94
CAS:1131456-28-4
Purity:≥98% Package:1g,5g,10g,25g根据客户需要分装 Remarks:Not For Human Use, Lab Use Only.
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| Company Name: |
ShangHai Biochempartner Co.,Ltd
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| Tel: |
17754423994 17754423994 |
| Email: |
2853530910@QQ.com |
| Products Intro: |
Product Name:KGP94
CAS:1131456-28-4
Purity:98% HPLC LCMS Package:100mg;500mg;1g
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| Product Name: | KGP-94 | | Synonyms: | Hydrazinecarbothioamide, 2-[(3-bromophenyl)(3-hydroxyphenyl)methylene]-;KGP-94;Inhibitor,M2 marker,KGP94,Metastasis,Raw264.7 macrophage,metastatic carcinoma,Cathepsin,inhibit,prostate (PC-3ML),Cathepsin L,breast cancer cell;2-((3-Bromophenyl)(3-hydroxyphenyl)methylene)hydrazine-1-carbothioamide | | CAS: | 1131456-28-4 | | MF: | C14H12BrN3OS | | MW: | 350.23 | | EINECS: | | | Product Categories: | APIS | | Mol File: | 1131456-28-4.mol |  |
| | KGP-94 Chemical Properties |
| storage temp. | Store at -20°C | | form | Solid | | color | White to off-white |
| | KGP-94 Usage And Synthesis |
| Biological Activity | KGP94 is a selective inhibitor of cathepsin L with an IC50 of 189 nM[1]. KGP94 inhibits migration and invasion of metastatic carcinoma and shows low cytotoxicity (GI50=26.9 μM) against various human cell lines[2].
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[3].KGP94 (25 μM, 24 h) impairs the incasive capacities of both prostate and breat cancer cells by 53% and 88%, respectively[4].KGP94 (25 μM, 24 h) suppresses secreted CTSL activity by 94% and 92% in PC-3ML and MDA-MB-231, repsectively[4].
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[5]. | | References | [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. |
| | KGP-94 Preparation Products And Raw materials |
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