5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione

Bezeichnung:5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione

CAS-Nr648450-29-7

Englisch Name:5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione

CBNumberCB72100624

SummenformelC12H7N3O2S

Molgewicht257.27

MOL-Datei648450-29-7.mol

5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione physikalisch-chemischer Eigenschaften

Dichte	1.553±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: soluble1mg/mL, clear (warmed)
pka	6.02±0.20(Predicted)
Aggregatzustand	powder
Farbe	, faint red to orange to dark brown

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26
WGK Germany	3
HS Code	2934100090

Gefahreninformationscode (GHS)

5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Verwenden
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.
Biologische Aktivität
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.
Einzelnachweise
[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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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