SD 0006

For research use only.

Catalog No.S6502

SD 0006 Chemical Structure

Molecular Weight(MW): 397.86

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).

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Biological Activity

Description 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).
Targets
p38α [1]
(Cell-free assay)
p38β [1]
(Cell-free assay)
0.016 μM 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[1].

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[1].

Protocol

Animal Research:

[1]

- Collapse
  • Animal Models: Male Sprague-Dawley rats
  • Dosages: 30 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 80 mg/mL (201.07 mM)
Ethanol 2 mg/mL (5.02 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 397.86
Formula

C20H20ClN5O2

CAS No. 271576-80-8
Storage powder
in solvent
Synonyms N/A
Smiles OCC(=O)N1CCC(CC1)C2=N[NH]C(=C2C3=NC=NC=C3)C4=CC=C(Cl)C=C4

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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p38 MAPK Signaling Pathway Map

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