B5779-5mg | CHIR 99021 trihydrochloride Clinisciences

Background

CHIR 99021 trihydrochloride is hydrochloride of CHIR 99021, which inhibits GSK-3α and GSK-3β with IC50 values of 10 nM and 6.7 nM. GSK-3 is a serine/threonine kinase, responsible for phosphorylating either the serine or threonine residues of its substrates. This phosphorylation process is involved in various key biological processes, including gene transcription, protein synthesis, cell signaling, cellular transport, proliferation, apoptosis, intracellular communication and glucose regulation.

References:

1. Ring DB, Johnson KW, Henriksen EJ, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes, 2003, 52(3): 588-595.

2. Pandey MK, DeGrado TR. Glycogen synthase kinase-3 (GSK-3)-targeted therapy and imaging. Theranostics, 2016, 6(4): 571-593.

3. Mussmann R, Geese M, Harder F, et al. Inhibition of GSK3 promotes replication and survival of pancreatic beta cells. Journal of Biological Chemistry, 2007, 282(16): 12030-12037.

Chemical Properties

Physical Appearance	Off White solid
Storage	Store at -20°C
M.Wt	574.72
Formula	C₂₂H₁₈Cl₂N₈·3HCl
Solubility	insoluble in EtOH; ≥21.87 mg/mL in DMSO; ≥32.45 mg/mL in H2O
Chemical Name	(Z)-6-((2-((E)-(4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2(1H)-ylidene)amino)ethyl)imino)-1,6-dihydropyridine-3-carbonitrile trihydrochloride
SDF	Download SDF
Canonical SMILES	CC(N1)=CN=C1C(C(C2=C(Cl)C=C(Cl)C=C2)=N/3)=CNC3=N/CC/N=C4C=CC(C#N)=CN/4.Cl.Cl.Cl
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment:[3]
Cell lines	INS-1E cells
Reaction Conditions	0 ~ 20 μM CHIR 99021 for 24 h incubation
Applications	CHIR 99021 increased the rate of proliferation of INS-1E cells in a dose-dependent manner, with the rate of proliferation reaching a maximum in the presence of 2.5 ~ 10 μM CHIR 99021. Moreover, CHIR 99021 also dose-dependently counteracted INS-1E cell death induced by high glucose and high palmitate.
Animal experiment:[1]
Animal models	Male ZDF rats with type 2 diabetes
Dosage form	16, 30 or 48 mg/kg Orally
Applications	In ZDF rats with type 2 diabetes, a single oral dose of CHIR 99021 at 30 mg/kg rapidly lowered plasma glucose, with a maximal reduction of nearly 150 mg/dl 3 ~ 4 hours after administration, while plasma insulin remained at or below control levels. Moreover, oral administration of CHIR 99021 at 16 or 48 mg/kg 1 hour before oral glucose challenges in ZDF rats substantially improved glucose tolerance, with 14% and 33% reduction in plasma glucose.
Note	The technical data provided above is for reference only.
	References: 1. Ring DB, Johnson KW, Henriksen EJ, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes, 2003, 52(3): 588-595. 2. Pandey MK, DeGrado TR. Glycogen synthase kinase-3 (GSK-3)-targeted therapy and imaging. Theranostics, 2016, 6(4): 571-593. 3. Mussmann R, Geese M, Harder F, et al. Inhibition of GSK3 promotes replication and survival of pancreatic beta cells. Journal of Biological Chemistry, 2007, 282(16): 12030-12037.

Quality Control

Purity = 98.59%

Chemical structure

CHIR 99021 trihydrochloride

Référence B5779-5mg

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