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KP-457

SKU: orb2279122

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).

Research Area

Protein Biochemistry

Images & Validation

Key Properties

CAS Number1365803-52-6
MW480.56
Purity98.33%
FormulaC21H24N2O7S2
SMILESC(CS(=O)(=O)C1=CC=C(OCC#CC)C=C1)(N(C=O)O)C2=CC=C(CNS(C)(=O)=O)C=C2
TargetMMP
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.32 mM);DMSO:100 mg/mL (208.09 mM)

Bioactivity

Target IC50
MMP3:9.760 μM|MMP13:0.93 μM|MMP14:2.14 μM|ADAM17:0.111 μM|MMP17:7.1 μM|MMP8:2.2 μM|MMP9:5.41 μM|ADAM10:0.748 μM|MMP2:0.717 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 durin the MK differentiation and thrombopoietic stages of HPC cultured at 37℃. 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. 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

Storage & Handling

Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
DisclaimerFor research use only

Alternative Names

ADAM17, KP 457, KP457, KP-457, TNF‐α‐converting enzyme
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Key Properties

No computed properties available.

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Protocol Information

KP-457 (orb2279122)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
¥ 1,820.00
5 mg
¥ 3,510.00
1 ml x 10 mM (in DMSO)
¥ 3,770.00
10 mg
¥ 5,460.00
25 mg
¥ 9,490.00
50 mg
¥ 14,690.00
100 mg
¥ 19,760.00
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