Description
Key facts
CAS number:252917-06-9,
Purity:>95%,
Form:LiquidSee storage information,
Molecular weight:465.3 Da,
Molecular formula:C22H18Cl2N8,
PubChem:9956119,
Nature:Synthetic,
Biochemical name:6-((2-((4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-yl)amino)ethyl)amino)nicotinonitrile,
Biological description:Potent, highly selective aminopyrimidine GSK3 inhibitor (IC50 values are 6.7 and 10 nM at GSK3β and GSK3α, respectively). Exhibits >500-fold selectivity for GSK3 against 20 closely related protein kinases and >800-fold selectivity for 23 additional enzymes and 22 receptors. Promotes self-renewal of mouse and human ESC due to β-catenin and c-Myc protein level stabilization. Commonly used in multiple stages of organoid generation.,
Canonical smiles:CC1=CN=C(N1)C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)Cl)NCCNC4=NC=C(C=C4)C#N,
InChi:InChI=1S/C22H18Cl2N8/c1-13-10-29-21(31-13)17-12-30-22(32-20(17)16-4-3-15(23)8-18(16)24)27-7-6-26-19-5-2-14(9-25)11-28-19/h2-5,8,10-12H,6-7H2,1H3,(H,26,28)(H,29,31)(H,27,30,32),
InChiKey:AQGNHMOJWBZFQQ-UHFFFAOYSA-N,
IUPAC Name:6-[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2-yl]amino]ethylamino]pyridine-3-carbonitrile
Product details:
CHIR99021 can be used in assays related to Cell Signalling, Apoptosis, Cancer Growth Inhibitors and Tyrosine Kinase Inhibitors.
The molecular weight of CHIR99021, Sterile-Filtered (ab291107) is 465.3 g/mol.
CHIR99021, Sterile-Filtered ab291107, (previously known as EZSolution CHIR99021, Sterile-Filtered, 1991) is a 10 mM (4.65 mg in 1 ml), sterile-filtered solution of the GSK-3β inhibitor CHIR99021 in anhydrous DMSO.
Properties and Storage Information:
Shipped at conditions-Blue Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C, Storage information-It is important to note that this is air sensitive and impurities can occur as a result of air oxidation, Store under desiccating conditions
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
Glycogen synthase kinase 3 beta or GSK3 beta is a serine/threonine protein kinase that regulates various cellular processes. It is also referred to as GSK3B and has a molecular weight of approximately 47 kilodaltons (kDa). This enzyme is widely expressed in many tissues with notably high expression levels in the brain. Mechanically GSK3 beta phosphorylates target proteins affecting their activity stability and interactions with other proteins.
Biological function summary
As an important regulatory protein GSK3 beta plays a role in multiple cellular functions including metabolism cell cycle and cell signaling. It often interacts with components in signaling complexes and modulates the activity of these complexes involving phosphorylation. It is involved in the regulation of transcription factors such as c-Myc and β-catenin influencing cell fate and survival. This ability to modulate diverse functions highlights GSK3 beta's importance in cellular regulation.
Pathways
GSK3 beta participates in significant signaling pathways such as the Wnt/β-catenin and insulin signaling pathways. In the Wnt pathway GSK3 beta phosphorylates β-catenin marking it for degradation which regulates gene transcription. In insulin signaling it interacts with proteins like AKT to mediate glycogen synthesis. These interactions highlight its role in maintaining cellular homeostasis and energy balance.
GSK3 beta has implications in Alzheimer's disease and type 2 diabetes. It is associated with tau protein hyperphosphorylation and neurofibrillary tangles in Alzheimer's disease. In diabetes its role in insulin signaling impacts glucose metabolism. Further GSK3 beta's dysfunction relates to disrupted signaling related to these conditions positioning it as a potential therapeutic target.
