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

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
1 mg USD 142 In-stock
5 mg USD 300 In-stock
10 mg USD 480 In-stock
25 mg USD 860 In-stock
50 mg USD 1350 In-stock
100 mg USD 1890 In-stock
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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  • Purity & Documentation

  • References

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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].

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

KGP94 Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8553 mL 14.2763 mL 28.5527 mL 71.3817 mL
5 mM 0.5711 mL 2.8553 mL 5.7105 mL 14.2763 mL
10 mM 0.2855 mL 1.4276 mL 2.8553 mL 7.1382 mL
15 mM 0.1904 mL 0.9518 mL 1.9035 mL 4.7588 mL
20 mM 0.1428 mL 0.7138 mL 1.4276 mL 3.5691 mL
25 mM 0.1142 mL 0.5711 mL 1.1421 mL 2.8553 mL
30 mM 0.0952 mL 0.4759 mL 0.9518 mL 2.3794 mL
40 mM 0.0714 mL 0.3569 mL 0.7138 mL 1.7845 mL
50 mM 0.0571 mL 0.2855 mL 0.5711 mL 1.4276 mL
60 mM 0.0476 mL 0.2379 mL 0.4759 mL 1.1897 mL
80 mM 0.0357 mL 0.1785 mL 0.3569 mL 0.8923 mL
100 mM 0.0286 mL 0.1428 mL 0.2855 mL 0.7138 mL
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KGP94 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KGP941131456-28-4KGP 94KGP-94CathepsinMetastasisCathepsin LMDA-MB-231breast cancer cellprostate (PC-3ML)M2 markerRaw264.7 macrophagemetastatic carcinomaInhibitorinhibitorinhibit

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