SD 0006

Catalog No.S6502 Batch:S650201

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Technical Data

Formula

C20H20ClN5O2
Molecular Weight 397.86 CAS No. 271576-80-8
Solubility (25°C)* In vitro DMSO 80 mg/mL (201.07 mM)
Ethanol 2 mg/mL (5.02 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Animal Study:

[1]
  • Animal Models

    Male Sprague-Dawley rats

  • Dosages

    30 mg/kg

  • Administration

    oral

Selleck's SD 0006 has been cited by 1 publication

SD0006 promotes nucleus pulposus cell proliferation via the p38MAPK/HDAC4 pathway [ Eur Rev Med Pharmacol Sci, 2020, 24(21):10966-10974] PubMed: 33215410

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.