KGP-94
- CAS No.
- 1131456-28-4
- Chemical Name:
- KGP-94
- Synonyms
- KGP-94;Hydrazinecarbothioamide, 2-[(3-bromophenyl)(3-hydroxyphenyl)methylene]-;2-((3-Bromophenyl)(3-hydroxyphenyl)methylene)hydrazine-1-carbothioamide;Inhibitor,M2 marker,KGP94,Metastasis,Raw264.7 macrophage,metastatic carcinoma,Cathepsin,inhibit,prostate (PC-3ML),Cathepsin L,breast cancer cell
- CBNumber:
- CB23383793
- Molecular Formula:
- C14H12BrN3OS
- Molecular Weight:
- 350.23
- MDL Number:
- MOL File:
- 1131456-28-4.mol
KGP-94 Chemical Properties,Uses,Production
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
Raw materials
Preparation Products
KGP-94 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd. | 17702719238 17702719238 | sales@sun-shinechem.com | China | 922 | 64 |
| Tianjin Kailiqi Biotechnology Co., Ltd. | 15076683720 | klq@cw-bio.com | China | 3717 | 55 |
| ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8011 | 62 |
| Wuhan Sun-shine Bio-technology Corporation Limited | +86-027-6552-2453 | sales@sun-shinechem.com | China | 727 | 58 |
| Nanjing Meihao Pharmaceutical Technology Co., Ltd. | meitaochem@126.com | meitaochem@126.com | China | 19105 | 58 |
| Zhengzhou convergence chemical co., LTD | 0371-0371-55153829 18003835034 | 2853979819@qq.com | China | 9273 | 58 |
| Bide Pharmatech Ltd. | 400-1647117 15221909166 | product02@bidepharm.com | China | 63720 | 58 |
| InvivoChem | 13549236410 | sales@invivochem.cn | China | 6749 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24017 | 58 |