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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
Last updated:2024-07-02 08:55:03

KGP-94 Properties

storage temp. Store at -20°C
form Solid
color White to off-white

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

Global( 12)Suppliers
Supplier Tel Email 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

KGP-94 Spectrum

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 1131456-28-4 APIS