601514-19-6 Usage
Description
GSK-3BETA INHIBITOR XII, also known as TWS119, is a cell-permeable and potent inhibitor of glycogen synthase kinase-3β (GSK-3β) with an IC50 value of 30 nM. It exhibits high affinity for GSK-3β (Kd = 126 nM) and leads to an increase in the level of β-catenin, a downstream substrate of GSK-3β in the Wnt signaling pathway. GSK-3BETA INHIBITOR XII has been shown to selectively induce neuronal differentiation in both pluripotent murine embryonal carcinoma cells (P19; 30-40% at 1 μM) and embryonic stem cells (D3; 50-60% at 400 nM).
Uses
Used in Pharmaceutical Industry:
GSK-3BETA INHIBITOR XII is used as an ARMS-selective inhibitor for targeting GSK-3β, which plays a crucial role in various cellular processes, including glycogen metabolism, cell cycle regulation, and protein synthesis. Its inhibition can lead to potential therapeutic benefits in treating various diseases.
Used in Neuroscience Research:
GSK-3BETA INHIBITOR XII is used as a research tool for promoting neuronal differentiation in both pluripotent murine embryonal carcinoma cells (P19) and embryonic stem cells (D3). This application aids in understanding the role of GSK-3β in neuronal development and may contribute to the development of treatments for neurodegenerative diseases.
Used in Drug Development:
TWS119, as a GSK-3β inhibitor, is used in the development of novel therapeutics targeting the Wnt signaling pathway. By modulating the levels of β-catenin, this inhibitor can potentially be utilized in the treatment of various diseases, including cancer, where the Wnt pathway is often dysregulated.
Biological Activity
Inhibitor of glycogen synthase kinase-3 β (IC 50 = 30 nM). Induces neuronal differentiation in pluripotent murine embryonal carcinoma cells and embryonic stem cells (ESCs).
Biochem/physiol Actions
TWS119 favors the γδT cells survival and proliferation by activating the mammalian target of rapamycin (mTOR) pathway. It also promotes the expression of T-cell factor 1 (TCF1) and modulates cytokine production.
references
[1] ding s, wu t y h, brinker a, et al. synthetic small molecules that control stem cell fate. proceedings of the national academy of sciences, 2003, 100(13): 7632-7637.[2] wu t y h, ding s. applying chemical tools to the discovery of novel regenerative medicine. drug discovery today: technologies, 2006, 3(3): 255-260.
Check Digit Verification of cas no
The CAS Registry Mumber 601514-19-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 6,0,1,5,1 and 4 respectively; the second part has 2 digits, 1 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 601514-19:
(8*6)+(7*0)+(6*1)+(5*5)+(4*1)+(3*4)+(2*1)+(1*9)=106
106 % 10 = 6
So 601514-19-6 is a valid CAS Registry Number.
InChI:InChI=1/C18H14N4O2/c19-12-4-1-3-11(7-12)16-9-15-17(22-16)20-10-21-18(15)24-14-6-2-5-13(23)8-14/h1-10,23H,19H2,(H,20,21,22)
601514-19-6Relevant articles and documents
Efficient formation of 4,6-disubstituted pyrrolo[2,3-d]pyrimidines: A novel route to TWS119, a glycogen synthase kinase-3β inhibitor
Mayasundari, Anand,Fujii, Naoaki
supporting information; experimental part, p. 3597 - 3598 (2010/08/19)
A concise synthesis of 4,6-disubstituted pyrrolo[2,3-d]pyrimidines is described. The key step involves the formation of an ether or thioether linkage along with concurrent ring closure in one-pot to yield the desired product in only two steps from a common intermediate. The reaction is chemoselective to incorporate phenol, thiophenol, and thiol. This method enabled efficient production of TWS119, a glycogen synthase kinase-3β inhibitor.
