1. Metabolic Enzyme/Protease
  2. Cathepsin
  3. KGP94

KGP94 

Cat. No.: HY-118762 Purity: 99.53%
COA Handling Instructions

KGP94 is a selective inhibitor of cathepsin L with an IC50 of 189 nM. KGP94 inhibits migration and invasion of metastatic carcinoma and shows low cytotoxicity (GI50=26.9 µM) against various human cell lines.

For research use only. We do not sell to patients.

KGP94 Chemical Structure

KGP94 Chemical Structure

CAS No. : 1131456-28-4

Size Price Stock Quantity
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
25 mg USD 860 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1890 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

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].

IC50 & Target

189 nM (cathepsin L)[1]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Invasion Assay[4]

Cell Line: PC-3ML, MDA-MB-231
Concentration: 10 μM, 25 μM
Incubation Time: 24 hours
Result: Attenuated migration and invasion of prostate and breast cancer cells.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

350.23

Formula

C14H12BrN3OS

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (285.53 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8553 mL 14.2763 mL 28.5527 mL
5 mM 0.5711 mL 2.8553 mL 5.7105 mL
10 mM 0.2855 mL 1.4276 mL 2.8553 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.14 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.14 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Product Name:
KGP94
Cat. No.:
HY-118762
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