648450-29-7 Usage
Description
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione is a chemical compound with a complex molecular structure, characterized by its quinoxalinylmethylene and thiazolidinedione moieties. It is a derivative of thiazolidinedione, which is known for its diverse biological activities and potential applications in various fields.
Uses
Used in Pharmaceutical Industry:
5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione is used as a phosphatidylinositol 3-kinase (PI3K) inhibitor for various applications, including the study of Rab5-positive early endosome (EE) vesicles. Its ability to inhibit PI3K makes it a valuable tool in understanding the role of this enzyme in cellular processes and its potential as a therapeutic target.
Used in Immunology Research:
In the field of immunology, 5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione is used as a PI3K inhibitor to treat splenocytes for graft-versus-host disease (GVHD) induction. GVHD is a severe complication that can occur after bone marrow transplantation, and this compound may help modulate the immune response to prevent or treat the condition.
Used in Cellular Biology:
As a class 1A PI3K inhibitor, 5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione is employed to treat CD4+ T cells. CD4+ T cells play a crucial role in the immune system, and modulating their activity with PI3K inhibitors can provide insights into the regulation of immune responses and the development of novel therapeutic strategies for various diseases.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 648450-29-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 6,4,8,4,5 and 0 respectively; the second part has 2 digits, 2 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 648450-29:
(8*6)+(7*4)+(6*8)+(5*4)+(4*5)+(3*0)+(2*2)+(1*9)=177
177 % 10 = 7
So 648450-29-7 is a valid CAS Registry Number.
InChI:InChI=1/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+
