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KP-457

🥰Excellent
Catalog No. T77778Cas No. 1365803-52-6
Alias KP457, KP 457

KP-457 is a specific inhibitor of a disintegrin-metalloproteinase 17 (ADAM17) and a TNFα converting enzyme TACE inhibitor that blocks the production of soluble TNF (sTNF).

KP-457

KP-457

🥰Excellent
Purity: 98.33%
Catalog No. T77778Alias KP457, KP 457Cas No. 1365803-52-6
KP-457 is a specific inhibitor of a disintegrin-metalloproteinase 17 (ADAM17) and a TNFα converting enzyme TACE inhibitor that blocks the production of soluble TNF (sTNF).
Pack SizePriceAvailabilityQuantity
1 mg$93In Stock
5 mg$228In Stock
10 mg$372In Stock
25 mg$689In Stock
50 mg$1,090In Stock
100 mg$1,480In Stock
1 mL x 10 mM (in DMSO)$243In Stock
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Purity:98.33%
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Product Introduction

Bioactivity
Description
KP-457 is a specific inhibitor of a disintegrin-metalloproteinase 17 (ADAM17) and a TNFα converting enzyme TACE inhibitor that blocks the production of soluble TNF (sTNF).
Targets&IC50
MMP2:0.717 μM, ADAM10:0.748 μM, MMP9:5.41 μM, MMP17:7.1 μM, MMP8:2.2 μM, MMP13:0.93 μM, ADAM17:0.111 μM, MMP14:2.14 μM, MMP3:9.760 μM
In vitro
b>METHODS: The ability of KP-457 (15 μM) to inhibit GPIbα shedding during in vitro generation of iPSC platelets was studied when administered during the MK differentiation and thrombopoietic stages of HPC cultured at 37°C.
RESULTS: KP-457 had no significant effect on MK numbers; retention of GPIbα by KP-457 was consistently observed in platelets derived from human embryonic stem cells and imMKCLs. [1]
KP-457 is a selective metalloproteinase 17 (ADAM17) inhibitor, with selectivity for ADAM17 over other MMPs and ADAM10, with IC50 values ​​of 0.011 μM (ADAM17), 0.748 μM (ADAM10), 0.717 μM (MMP2), 9.760 μM (MMP3), 2.2 μM (MMP8), 5.41 μM (MMP9), 0.93 μM (MMP13), 2.140 μM (MMP14), and 7.1 μM (MMP17), respectively. [1]
AliasKP457, KP 457
Chemical Properties
Molecular Weight480.56
FormulaC21H24N2O7S2
Cas No.1365803-52-6
SmilesC(CS(=O)(=O)C1=CC=C(OCC#CC)C=C1)(N(C=O)O)C2=CC=C(CNS(C)(=O)=O)C=C2
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (208.09 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0809 mL10.4045 mL20.8091 mL104.0453 mL
5 mM0.4162 mL2.0809 mL4.1618 mL20.8091 mL
10 mM0.2081 mL1.0405 mL2.0809 mL10.4045 mL
20 mM0.1040 mL0.5202 mL1.0405 mL5.2023 mL
50 mM0.0416 mL0.2081 mL0.4162 mL2.0809 mL
100 mM0.0208 mL0.1040 mL0.2081 mL1.0405 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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