| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H17Cl2N9O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor, with IC50 values of 0.65 nM for GSK-3α and 0.58 nM for GSK-3β, and it shows less potent activity against cdc2 and erk2. It is supplied as a light yellow to yellow solid (C20H17Cl2N9O2, MW 486.31) at 98.44% purity.
Physical & Chemical Properties
| CAS Number | 252935-94-7 |
|---|---|
| Molecular Formula | C20H17Cl2N9O2 |
| Molecular Weight | 486.31 g/mol |
| Purity | 98.44% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | ClC1=CC(Cl)=CC=C1C2=NC(NCCNC3=CC=C([N+]([O-])=O)C(N)=N3)=NC=C2N4C=CN=C4 |
| Target | GSK-3β, GSK-3α, cdc2 |
| Signaling Pathway | PI3K/Akt/mTOR; Stem Cell/Wnt |
| Solubility | In Vitro: DMSO: 12.5 mg/mL (25.70 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
GSK-3β 0.58 nM (IC50) |
GSK-3α 0.65 nM (IC50) |
cdc2 3700 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 12.5 mg/mL (25.70 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
CHIR 98014 inhibits human GSK-3β with a Ki value of 0.87 nM. CHIR 98014 stimulates GS in CHO-IR cells and rat hepatocytes (EC50s: 106 nM and 107 nM, respectively)[1]. CHIR-98014 (1 μM) lowers the viability of ES-CCE cells by 52%, with an IC50 of 1.1 μM. In addition, combining CHIR-98014 with CHIR-99021 significantly activates the Wnt/beta-catenin pathway in ES-D3 cells. T gene expression is induced up to 2,500-fold in CHIR-98014 treated cells. CHIR-98014 (1 μM) also yields around 50% Brachyury-positive cells, with an EC50 of 0.32 μM[2]. CHIR98014 (10 μM) protects cortical and hippocampal neurons from the neurite loss caused by 20 μM PrP1-30, and substantially reduces the number of dead cells[3].
In Vivo
In markedly diabetic and insulin-resistant db/db mice, CHIR 98014 (30 mg/kg, i.p.) significantly reduces fasting hyperglycemia within 4 h of treatment and improves glucose disposal during an ipGTT[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[2]
Determine the viability of mouse ES cells by MTT assay after three days of exposure to different concentrations of GSK3 inhibitors. A decrease in MTT activity is a reliable metabolism-based measure of cell viability and correlates with the loss of viability. Seed 2,000 cells overnight on gelatin-coated 96-well plates in LIF-containing ES cell medium. The next day, switch to medium without LIF and with reduced serum, add 0.1-1 μM BIO, or 1-10 μM SB-216763, CHIR-99021 or CHIR-98014. Use basal medium without GSK3 inhibitors or DMSO as control. Analyze all tested conditions in triplicates[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Derivation of totipotent-like stem cells with blastocyst-like structure forming potential. Cell Res 2022 Jun;32(6):513-529. PMID: 35508506
A GYS2/p53 Negative Feedback Loop Restricts Tumor Growth in HBV-Related Hepatocellular Carcinoma. Cancer Res 2019 Feb 1;79(3):534-545.
PDZK1-ULK1 Axis Triggers Lipophagy to Inhibit Tumor Progression and Sunitinib Resistance in Clear Cell Renal Cell Carcinoma. Adv Sci (Weinh) 2026 Apr;13(23):e11606. PMID: 41698049
Caspase-3/7 deficiency results in enhanced intestinal inflammation and reduced tumorigenesis. Sci Adv 2026 Mar 20;12(12):eadz5906. PMID: 41861024
A PTX3/TLR4 axis sustains SHH-Medulloblastoma growth and defines a new therapeutic vulnerability. Neuro Oncol 2026 Jul 23:noag167. PMID: 42494116
Development of a live cell assay for real-time monitoring the interactions between the Hippo pathway components 14-3-3 and TAZ. SLAS Discov 2024 Nov 5;29(8):100191. PMID: 39510350
Mechanistic insights into AKT1/GSK3β/CD36 axis regulation in ZLY06-induced hepatic lipid metabolism dysfunction and protective intervention via AKT activation strategies. Food Chem Toxicol 2025 Oct:204:115628. PMID: 40633829
β-Sitosterol alleviates the malignant phenotype of hepatocellular carcinoma cells via inhibiting GSK3B expression. Hum Cell 2024 Jul;37(4):1156-1169. PMID: 38814517
SSRN. 2025 Jul 25.
bioRxiv. 2024 September 07.
