AS-605420 is an orally-available, ATP competitive inihbitor of the thiazolinedione class with IC50 potency against PI3Kg of 8 nM. It also has peripheral activity versus other PI3K isoforms of 60 nM, 270 nM, and 300 nM for alpha, beta, and delta, respectively.AS-605240 has been shown to selectively block class IB PI3K signaling in cultured macrophages. Dose-dependent treatment resulted in lowered blood glucose levels with improvement in insulin sensitivity and glucose tolerance without adverse effect on body weight. [1]AS-605240 has also been utilized in the exploration for experimental autoimmune encephalomyelitis (EAE). AS605420-treated mice fully recovered from EAE and experienced significantly reduced clinical and cumulative disease scores. Histological CNS analysis revealed that AS605240 treated mice had reduced cellular pathology in the spinal cord and reduced signs of demyelination. [2]
Technical information:
| Chemical Formula: | C12H7N3O2S | |
| CAS #: | 648450-29-7 | |
| Molecular Weight: | 257.27 | |
| Purity: | >98% | |
| Appearance: | Grey | |
| Chemical Name: | (Z)-5-(quinoxalin-6-ylmethylene)thiazolidine-2,4-dione | |
| Solubility: | Up to 5 mM in DMSO | |
| Synonyms: | AS-605240, AS 605240, AS605240 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Kobayashi et al., Blockade of class IB phosphoinositide-3 kinase ameliorates obesity-induced inflammation and insulin resistance. Proc. Natl. Acad. Sci. 2011, 108(14), 5753-5758. Pubmed ID:21436039 |
| 2. | Comerford et al., PI3K? drives priming and survival of autoreactive CD4(+) T cells during experimental autoimmune encephalomyelitis. PLoSONE, 2012, 7(9), e45095 Pubmed ID:23028778 |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
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