1. Metabolic Enzyme/Protease
  2. MMP

KP-457 

Cat. No.: HY-110397 Purity: 98.78%
Handling Instructions

KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and 5050s 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
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3300 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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 5050s 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

IC50: 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), 7100 nM (MMP17)[1]

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].

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].

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (260.12 mM; Need ultrasonic)

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
10 mM 0.2081 mL 1.0405 mL 2.0809 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

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

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

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
Molecular Weight

480.55

Formula

C₂₁H₂₄N₂O₇S₂

CAS No.

1365803-52-6

SMILES

CS(=O)(NCC1=CC=C(C(N(C=O)O)CS(=O)(C2=CC=C(OCC#CC)C=C2)=O)C=C1)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
KP-457
Cat. No.:
HY-110397
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KP-457

Cat. No.: HY-110397