KGP94

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].

Product Specifications

CAS Number

[1131456-28-4]

UNSPSC

12352005

Hazard Statement

H301

Target

Cathepsin

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/kgp94.html

Purity

99.77

Solubility

DMSO : ≥ 100 mg/mL

Smiles

S=C(N/N=C(C1=CC(O)=CC=C1)\C2=CC(Br)=CC=C2)N

Molecular Formula

C14H12BrN3OS

Molecular Weight

350.23

Precautions

H301

References & Citations

[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.|[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.