2. Metabolic Enzyme/Protease
  3. MMP
  4. KP-457

KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.

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

KP-457 Chemical Structure

KP-457 Chemical Structure

CAS No. : 1365803-52-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 296 In-stock
Solution
10 mM * 1 mL in DMSO USD 296 In-stock
Solid
5 mg USD 280 In-stock
10 mg USD 450 In-stock
25 mg USD 850 In-stock
50 mg USD 1350 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of KP-457:

KP-457 Related Antibodies

Top Publications Citing Use of Products

View All MMP Isoform Specific Products:

View All Isoforms
MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.

IC50 & Target[1]

ADAM17

11.1 nM (IC50)

ADAM10

748 nM (IC50)

MMP2

717 nM (IC50)

MMP13

930 nM (IC50)

MMP14

2140 nM (IC50)

MMP8

2200 nM (IC50)

MMP9

5410 nM (IC50)

MMP17

7100 nM (IC50)

MMP3

9760 nM (IC50)

In Vitro

KP-457 is a selective metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively. KP-457 blocks Zn2+ chelation of the catalytic domain of ADAM17. KP-457 (15 μM) retains the expression of GPIbα on iPSC-derived platelets[1].

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

KP-457 Related Antibodies
In Vivo

In a thrombus formation model using immunodeficient mice after platelet transfusion, induced pluripotent stem cells (iPSCs) platelets generated with KP-457 exerts good hemostatic function[1].

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

480.55

Formula

C21H24N2O7S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CS(=O)(NCC1=CC=C(C(N(C=O)O)CS(=O)(C2=CC=C(OCC#CC)C=C2)=O)C=C1)=O
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 : 125 mg/mL (260.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0809 mL 10.4047 mL 20.8095 mL
5 mM 0.4162 mL 2.0809 mL 4.1619 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: ≥ 2.08 mg/mL (4.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

Purity: 99.18%

SDS (392 KB)

COA (251 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

Briefly, 3 × 104 hematopoietic progenitor cells (HPCs) derived from iPS-sacs on C3H10T1/2 feeder cells in the presence of 20 ng/mL vascular endothelial growth factor are transferred on day 14 of culture onto C3H10T1/2 feeder cells in differentiation medium supplemented with 50 ng/mL stem cell factor, 100 ng/mL thrombopoietin, 25 U/mL heparin sodium, and KP-457 at 24°C or 37°C. The medium is refreshed every 3 days, and nonadherent cells are collected and analyzed on days 22-24[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 2.0809 mL 10.4047 mL 20.8095 mL 52.0237 mL
5 mM 0.4162 mL 2.0809 mL 4.1619 mL 10.4047 mL
10 mM 0.2081 mL 1.0405 mL 2.0809 mL 5.2024 mL
15 mM 0.1387 mL 0.6936 mL 1.3873 mL 3.4682 mL
20 mM 0.1040 mL 0.5202 mL 1.0405 mL 2.6012 mL
25 mM 0.0832 mL 0.4162 mL 0.8324 mL 2.0809 mL
30 mM 0.0694 mL 0.3468 mL 0.6936 mL 1.7341 mL
40 mM 0.0520 mL 0.2601 mL 0.5202 mL 1.3006 mL
50 mM 0.0416 mL 0.2081 mL 0.4162 mL 1.0405 mL
60 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8671 mL
80 mM 0.0260 mL 0.1301 mL 0.2601 mL 0.6503 mL
100 mM 0.0208 mL 0.1040 mL 0.2081 mL 0.5202 mL
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KP-457 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:

KP-4571365803-52-6KP457KP 457MMPMatrix metalloproteinasesInhibitorinhibitorinhibit

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