Home MAPK p38 MAPK inhibitor SD 0006

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SD 0006 p38 MAPK inhibitor

Cat.No.S6502

SD0006 is an inhibitor of p38 kinase-alpha (p38alpha) with IC50 values of 0.016 μM and 0.677 μM for p38α and p38β. It is selective for p38α kinase over 50 other kinases screened (including p38γ and p38δ with modest selectivity over p38β).
SD 0006 p38 MAPK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 397.86

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Quality Control

Batch: S650201 DMSO]80 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 99.49%
99.49

Solubility

In vitro
Batch:

DMSO : 80 mg/mL (201.07 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 397.86 Formula

C20H20ClN5O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 271576-80-8 -- Storage of Stock Solutions

Synonyms N/A Smiles C1CN(CCC1C2=C(C(=NN2)C3=CC=C(C=C3)Cl)C4=NC=NC=C4)C(=O)CO

Mechanism of Action

Targets/IC50/Ki
p38α
(Cell-free assay)
0.016 μM
p38β
(Cell-free assay)
0.677 μM
In vitro

SD0006 is selective for p38α kinase over 50 other kinases screened (including p38γ and p38δ with modest selectivity over p38β). It suppresses Inflammatory mediator release in cellular studies. SD0006 suppresses expression of multiple proinflammatory proteins at both the transcriptional and translational levels. In RASFs, SD0006 has no direct inhibitory activity against COX-1 or COX-2, yet it could completely inhibit in a dose-dependent manner the release of IL-1β-stimulated PGE2 with an IC50 of 96.2 nmol/l.
In vivo

In vivo, SD0006 is effective in animal models of chronic inflammation and disease. It is effective in the rat streptococcal-cell-wall-induced arthritis model, with dramatic protective effects on paw joint integrity and bone density. SD0006 also demonstrates good oral anti-inflammatory efficacy with excellent cross-species correlation between the rat, cynomolgus monkey, and human. It alleviates swelling and pain in a rodent acute inflammation model.
References

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