A0233
AS605240
≥98% (HPLC)
别名:
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione
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关于此项目
经验公式（希尔记法）:
C12H7N3O2S
化学文摘社编号:
分子量:
257.27
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
AS605240, ≥98% (HPLC)
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)/b10-6-
SMILES string
O=C1NC(=O)C(\S1)=C\c2ccc3nccnc3c2
InChI key
SQWZFLMPDUSYGV-POHAHGRESA-N
assay
≥98% (HPLC)
form
powder
color
, faint red to orange to dark brown
solubility
DMSO: 1 mg/mL, clear (warmed)
storage temp.
2-8°C
Quality Level
Application
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.
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.
AS605240 is a potent and selective PI3Kγ inhibitor.
Features and Benefits
This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Phosphoinositide Kinases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
Xinyi Yu et al.
Scientific reports, 8(1), 10988-10988 (2018-07-22)
Chronic kidney disease (CKD) poses a formidable challenge for public healthcare worldwide as vast majority of patients with CKD are also at risk of accelerated cardiovascular disease and death. Renal fibrosis is the common manifestation of CKD that usually leads
Irene Filippi et al.
Journal of cellular physiology, 229(12), 2067-2076 (2014-05-14)
Hypoxia represents an inadequate oxygen supply to tissues, which can modulate cell functions, primarily through the hypoxia-inducible transcription factor HIF-1α. Dendritic cells (DC) are professional antigen-presenting cells and their migration maybe affected by hypoxia, since the local microenvironment in lymphoid
Marina G M Castor et al.
Journal of leukocyte biology, 89(6), 955-964 (2011-03-16)
PI(3)Kγ is thought to mediate leukocyte migration to injured tissues and may be important in the pathogenesis of various T-lymphocyte-dependent pathologies, including autoimmune and inflammatory diseases. The present study evaluated the relevance of PI(3)Kγ in donor cells for the pathogenesis
Sen Shang et al.
Neuroscience, 415, 107-120 (2019-06-14)
The intense and prolonged inflammatory response after ischemic stroke significantly contributes to the secondary neural injury. PI3Kγ, which is involved in the regulation of vascular permeability, chemotactic leukocyte migration and microglia activation, is a key target for intervention in the
Xin Wei et al.
Biochemical and biophysical research communications, 397(2), 311-317 (2010-06-01)
Phosphoinositide 3-kinase-gamma (PI3Kgamma) has been identified to play the critical roles in inflammatory cells activation and recruitment in multiply inflammatory diseases and it promised to be a prospective target for relevant inflammatory diseases therapy. AS605240, a selective PI3Kgamma inhibitor, has
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