| Identification | Back Directory | [Name]
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione | [CAS]
648450-29-7 | [Synonyms]
AS605240
AS-605240, >=98%
AS-605240(AS 605240)
PI 3-Kinase Inhibitor (AS605240)
PI 3-Kinase Inhibitor (AS605240) B-0301
AS-605240, 98%, a specific inhibitor of PI3Kγ
PI 3-Kγ Inhibitor - CAS 648450-29-7 - Calbiochem
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione
5-(Quinoxalin-6-ylmethylene)thiazolidine-2,4-dione
2,4-Thiazolidinedione, 5-(6-quinoxalinylMethylene)-
5-(6-Quinoxalinylmethylene)-2,4-thiazolidine-2,4-dione
(Z)-5-(quinoxalin-6-ylmethylene)thiazolidine-2,4-dione
(E)-5-(quinoxalin-6-ylMethylene)thiazolidine-2,4-dione
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione USP/EP/BP
AS 605240,5-(6-Quinoxalinylmethylene)-2,4-thiazolidine-2,4-dione
AS-605240
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione AS-605240 | [Molecular Formula]
C12H7N3O2S | [MDL Number]
MFCD11100415 | [MOL File]
648450-29-7.mol | [Molecular Weight]
257.27 |
| Chemical Properties | Back Directory | [density ]
1.553±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble1mg/mL, clear (warmed) | [form ]
powder | [pka]
6.02±0.20(Predicted) | [color ]
, faint red to orange to dark brown | [InChI]
InChI=1S/C12H7N3O2S/c16-11-10(18-12(17)15-11)6-7-1-2-8-9(5-7)14-4-3-13-8/h1-6H,(H,15,16,17) | [InChIKey]
SQWZFLMPDUSYGV-UHFFFAOYSA-N | [SMILES]
S1C(=CC2=CC=C3C(=C2)N=CC=N3)C(=O)NC1=O |
| Hazard Information | Back Directory | [Uses]
Potent, cell permeable and ATP-competitive inhibitor of phosphoinositide 3-kinase γ (PI(3)Kγ). Exhibits selectivity over other PI(3)K isoforms. | [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. |
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