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| | 5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione Basic information |
| | 5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione Chemical Properties |
| density | 1.553±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: soluble1mg/mL, clear (warmed) | | pka | 6.02±0.20(Predicted) | | form | powder | | color | , faint red to orange to dark brown |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26 | | WGK Germany | 3 | | HS Code | 2934100090 |
| | 5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione Usage And Synthesis |
| Uses | 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.
| | Definition | ChEBI: (5Z)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolidine-2,4-dione is a quinoxaline derivative that is quinoxaline in which the hydrogen at position 6 is replaced by a (2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl group. It is a potent inhibitor of the PI3Kgamma, with an IC50 of 8 nM and inhibits the progression of joint inflammation and damage in both lymphocyte-independent and dependent mouse models of rheumatoid arthritis. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor, an anti-inflammatory agent and an antirheumatic drug. It is a quinoxaline derivative and a member of thiazolidinediones. | | Biological Activity | 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. | | references | [1]. camps m, rückle t, ji h, et al. blockade of pi3kγ suppresses joint inflammation and damage in mouse models of rheumatoid arthritis[j]. nature medicine, 2005, 11(9): 936-943.
[2]. marone r, cmiljanovic v, giese b, et al. targeting phosphoinositide 3-kinase—moving towards therapy[j]. biochimica et biophysica acta (bba)-proteins and proteomics, 2008, 1784(1): 159-185. |
| | 5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione Preparation Products And Raw materials |
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