KGP-94 manufacturers
- KGP94
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- $63.00
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2026-07-27
- CAS:1131456-28-4
- Purity: 99.60%
- Supply Ability: 10g
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| Product Name: | KGP-94 | | Synonyms: | KGP-94;Hydrazinecarbothioamide, 2-[(3-bromophenyl)(3-hydroxyphenyl)methylene]-;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;K P-94;KGP94, 10 mM in DMSO | | 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 |
| Uses | 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]. | | 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]. | | in vivo | 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]. | Animal Model: | NCR nu/nu male mice[5] | | 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. |
| | 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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