5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione
- Product Name
- 5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione
- CAS No.
- 648450-29-7
- Chemical Name
- 5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione
- Synonyms
- AS605240;AS-605240, >=98%;AS-605240(AS 605240);PI 3-Kinase Inhibitor (AS605240);PI 3-Kγ Inhibitor AS-605240 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
- CBNumber
- CB72100624
- Molecular Formula
- C12H7N3O2S
- Formula Weight
- 257.27
- MOL File
- 648450-29-7.mol
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
N-Bromosuccinimide Price
- Product number
- A0233
- Product name
- AS605240
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $97.8
- Updated
- 2024/03/01
- Product number
- 528106
- Product name
- PI 3-Kγ Inhibitor
- Packaging
- 5mg
- Price
- $303
- Updated
- 2024/03/01
- Product number
- 10007707
- Product name
- AS-605240
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 10007707
- Product name
- AS-605240
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $56
- Updated
- 2024/03/01
- Product number
- A0233
- Product name
- AS605240
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $234.8
- Updated
- 2024/03/01
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione Chemical Properties,Usage,Production
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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View Lastest Price from 5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione manufacturers
- Product
- 5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione 648450-29-7
- Price
- US $2.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2018-12-24