5-(6-キノキサリニルメチレン)-2,4-チアゾリジンジオン

使用

AS605240 has been used:

• as a phosphatidylinositol 3-kinase (PI3K) inhibitor to study its effect on Rab5-positive early endosome (EE) vesicles.
• as a (PI3K) inhibitor to treat splenocytes for graft-versus-host disease (GVHD) induction.
• as a class 1A PI3K inhibitor?to treat CD4⁺?T cells.

生物活性

Potent and selective inhibitor of PI 3-kinase γ (PI3K γ ) (IC 50 = 8 nM). Displays 30-fold selectivity over PI3K δ and PI3K β and 7.5-fold selectivity over PI3K α . Suppresses the progression of joint inflammation and damage in both lymphocyte-independent and lymphocyte-dependent mouse models of rheumatoid arthritis. Orally active and ATP-competitive.

Biochem/physiol Actions

AS605240 inhibits human recombinant phosphatidylinositol 3-kinase (PI3K) γ, α, β, and δ by competing with adenosine triphosphate (ATP). It plays a role in protecting injury following ischemic stroke. AS605240 also inhibits the activation of astrocytes under the influence of Interleukin-6 (IL-6) and its soluble receptor (sIL-6R). It reduces collagen deposition and prevents lung inflammation. AS605240 also inhibits the increase of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) expression instigated by bleomycin. It is effective in preventing pulmonary fibrosis by inhibiting the transforming growth factor β1 (TGF-β1) and T lymphocytes infiltration into lungs.