CHIR-98014

For research use only.

Catalog No.S2745 Synonyms: CT98014

21 publications

CHIR-98014 Chemical Structure

CAS No. 252935-94-7

CHIR-98014 is a potent GSK-3α/β inhibitor with IC50 of 0.65 nM/0.58 nM in cell-free assays, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.

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10mM (1mL in DMSO) USD 157 In stock
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Selleck's CHIR-98014 has been cited by 21 publications

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Biological Activity

Description CHIR-98014 is a potent GSK-3α/β inhibitor with IC50 of 0.65 nM/0.58 nM in cell-free assays, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.
Targets
GSK-3β [1]
(Cell-free assay)
GSK-3α [1]
(Cell-free assay)
0.58 nM 0.65 nM
In vitro

CHIR-98014 inhibits human GSK-3β with Ki of 0.87 nM. CHIR-98014 is very effective in preventing murine and rat GSK-3. Although CHIR-98014 acts as a simple competitive inhibitor of ATP binding, it displays from 500-fold to >1000-fold selectivity for GSK-3 versus 20 other protein kinases including Cdc2, ERK2, Tie-2 and KDR. CHIR-98014 prevents Cdc2 with IC50 of 3.7 μM. However, CHIR 98014 reveals similar ptoency against the highly homologous ɑ and β isoforms of GSK-3, it is noteworthy that it stronly discriminated between GSK-3 and its closest homologs CDC2 and ERK2. Exposure of insulin receptor-expressing CHO-IR cells or primary rat hepatocytes to increasing concentrations of inhibitor CHIR98014 results in a two- to three-fold stimulation of the GS activity ratio above basal. The concentrations of CHIR-98014 giving rise to half-maximal GS stimulation (EC50) is 106 nM and 107 nM for CHO-IR and rat hepatocytes, respectively. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BGC-823 Mlq3VJJwdGmoZYLheIlwdiCjc4PhfS=> NUnjd3ZrPTBibl2= M2jrO|Q5KGh? NXLnPXpM[WK{b3fheIVlKHKOTV:zJJBzd3SnaX6tbY5lfWOnZDDwdo9tcW[ncnH0bY9v NIrNeWgzQTR|Nk[wOi=>
HGC-27 NUjaVYR5WHKxbHnm[ZJifGmxbjDhd5NigQ>? NGrYO2w2OCCwTR?= NI[2doI1QCCq MYnhZpJw\2G2ZXSgdmxOVzNicILveIVqdi2rbnT1Z4VlKHC{b3zp[oVz[XSrb36= MYOyPVQ{PjZyNh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-GSK3β / GSK3β / β-catenin ; 

PubMed: 28415692     


(A) CHIR-98014 and TWS119 rescued the ethanol-induced suppressive effect on p-GSK3β and β-catenin in BMSCs. The western blot shows p-Akt-Ser473, total-Akt, p-GSK3β, total-GSK3β. (B) Western blot of β-catenin after 72 hours. β-actin served as internal reference. 

28415692
Growth inhibition assay
Cell viability; 

PubMed: 24779365     


Cell viability of mouse embryonic stem cells after exposure to GSK3 inhibitors. (A) Cell viability of the mouse embryonic stem cell line ES-D3 after a three day treatment with different concentrations of BIO, SB-216763, CHIR-99021 and CHIR-98014. Cell viability was measured with the MTT assay. DMSO without inhibitors was used as vehicle control. Data are expressed as percentages normalized to the control condition without inhibitors. (B) Cell viability of the mouse embryonic stem cell line ES-CCE after a three day treatment with different concentrations of BIO, SB-216763, CHIR-99021 and CHIR-98014. Values are means ± SEM, n = 3-5. ANOVA plus Dunnett’s post hoc test. ** p ≤ 0.01, * p ≤ 0.05 compared to the control.

24779365
In vivo GSK-3 inhibitor CHIR-98014 activates the GS activity ratio in isolated type I skeletal muscle from insulin-sensitive lean Zucker and from insulin-ressitant ZDF rats. Soleus muscle isolated from ZDF rats shows significant resistance to insulin for activation of GS but responded to 500 nM CHIR-98014 to the same extent (40% increase) as muscle from lean Zucker rats. Notably, GS activation by insulin plus CHIR-98014 is additive in muscle from lean Zucker rats and greater than additive in muscle from the ZDF rats. Total GS activity is not altered by either CHIR-98014 or insulin in these cells and muscles. Meanwhile, CHIR-98014 does not influence the insulin dose-response in muscle from lean animals. The reduction in hyperglycemia and improved glucose disposal are not limited to db/db mice and ZDF rats, as similar results are observed with ob/ob mice, diet-induced diabetic C57BL/6 mice, and glucose-intolerant SHHF rats treated with CHIR-98014. [1] Additionally, CHIR-98014 decreases the phosphorylation (Ser396) of tau protein in the cortex and hippocampus of postnatal rats. [2]

Protocol

Kinase Assay:

[1]

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Kinase assays:

Polypropylene 96-well plates are filled with 300 μL/well buffer (50 mM tris HCl, 10 mM MgCl2, 1 mM EGTA, 1 mM dithiothreitol, 25 mM β-glycerophosphate, 1 mM NaF, 0.01% BSA, pH 7.5) containing kinase, peptide substrate, and any activators. CHIR-98014 or controls are added in 3.5 μL of DMSO, followed by 50 μL of ATP stock to yield a final concentration of 1 μM ATP in all cell-free assays. After incubation, triplicate 100-μL aliquots are transferred to Combiplate eight plates containing 100 μL/well 50 μM ATP and 20 mM EDTA. After 1 hour, the wells are rinsed five times with PBS, filled with 200 μL of scintillation fluid, sealed, left 30 min, and counted in a scintillation counter. All steps are performed at room temperature.
Cell Research:

[1]

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  • Cell lines: CHO-IR cells
  • Concentrations: 0.01-10 μM
  • Incubation Time: 30 min
  • Method:

    CHO-IR cells expressing human insulin receptor are grown to 80% confluence in Hamm’s F12 medium with 10% fetal bovine serum and without hypoxanthine. Trypsinized cells are seeded in 6-well plates at 1 × 106 cells/well in 2 mL of medium without fetal bovine serum. After 24 hours, medium is replaced with 1 mL of serum-free medium containing GSK-3 inhibitor CHIR 98014 or control (final DMSO concentration 0.1%) for 30 min at 37 °C. Cells are lysed by freeze/thaw in 50 mM tris (pH 7.8) containing 1 mM EDTA, 1 mM DTT, 100 mM NaF, 1 mM phenylmethylsulfonyl fluoride, and 25 μg/mL leupeptin (buffer A) and centrifuged 15 min at 4 °C/14000 g. The activity ratio of GS is calculated as the GS activity in the absence of glucose-6-phosphate divided by the activity in the presence of 5 mM glucose-6-phosphate.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: db/db mice with 8-9 weeks
  • Dosages: 30 mg/kg
  • Administration: Subcutaneously
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 8 mg/mL warmed (16.45 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.
2mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 486.31
Formula

C20H17Cl2N9O2

CAS No. 252935-94-7
Storage powder
in solvent
Synonyms CT98014
Smiles C1=CC(=C(C=C1Cl)Cl)C2=NC(=NC=C2N3C=CN=C3)NCCNC4=NC(=C(C=C4)[N+](=O)[O-])N

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID