Products

Enzymes for Research, Diagnostic and Industrial Use

Products
Online Inquiry

Our Products Cannot Be Used As Medicines Directly For Personal Use.

24 hour
Promise

Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.

Skepinone-L

Cat No.
CEI-1528
Description
Skepinone-L is a selective inhibitor of p38 mitogen-activated protein kinase (MAPK) and TNF-α with IC50 values of 5 nM and 40 nM, respectively.
Product Overview
Skepinone-L is a selective inhibitor of p38 mitogen-activated protein kinase (MAPK) with IC50 value of 5 nM. P38 MAPKs are a class of MAPK which are responsive for stress stimuli, such as heat shock and osmotic shock. They are involved in cell differentiation and apoptosis. Skepinone-L is a ATP-competitive inhibitor of p38 MAPK. For in vitro test, the phosphory¬lation of heat shock protein 27 (HSP27) of the p38 MAPK pathway can be used as a marker to assess the activity of p38 MAPK. When HeLa cells were treated with anisomycin, skepinone-L showed dose-dependent inhibition of HSP27 phosphorylation with a cellular IC50-25 nM, which confirmed the inhibition of p38 MAPK. Additionally, in peripheral blood mononuclear cells (hPBMCs), treatment of skepinone-L resulted in the reduction of p38 MAPK downstream effectors including TNF-α, IL-1β and IL-10.In mouse model, oral administration of skepinone-L resulted in very high level of skepinone-L which was 240 nM and higher than the human whole-blood IC50 value of skepinone. Therefore, it resulted in the inhibition of TNF-α by 77% via the inhibition of upstream p38 MAPK. Thus, it demonstrated the pre¬eminent pharmacodynamic properties of skepinone-L.
CAS No.
1221485-83-1
Molecular Weight
425.42
Purity
0.98
Storage
Store at -20°C
Synonyms
Skepinone L
Targets
P38-MAPK
IC50
5 nM; 40 nM
Molecular Formula
C24H21F2NO4
Chemical Name
3-(2,4-difluoroanilino)-9-[(2R)-2,3-dihydroxypropoxy]-5,6-dihydrodibenzo[3,1-[7]annulen-11-one
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request

Our Products Cannot Be Used As Medicines Directly For Personal Use.

0
Click unfold / close
Inquiry Basket
Delete selected Quote Check Out
Decide to move out of the shopping cart?
Sure No, Back

Please choose product!

< Go Back
You have already added to buy this product