CHIR-98014
CHIR 98014 (CAS 252935-94-7) is a cell-permeable small molecule inhibitor, functioning as an inhibitor in kinase-related pathways and exhibiting potent inhibitory activity in various cellular targets. Additionally, it displays selectivity for specific kinase isoforms over other related kinases.
In experimental studies, CHIR 98014 inhibits kinase activity with an IC50 value of 0.65 nM and 0.58 nM, tested against purified kinase enzymes and relevant cell lines. Its action against cdc2 and related kinases is relatively weaker, indicating selectivity in its inhibitory profile. It can also suppress phosphorylation events downstream of its primary targets, thus modulating signal transduction pathways that are essential for cellular proliferation and differentiation.
In cell-based and biochemical assays, CHIR 98014 is widely used for the investigation of signaling pathways mediated by its target kinases. Researchers utilize this compound to study the effects of selective kinase inhibition on cellular processes such as cell cycle progression, apoptosis, and metabolic reprogramming. Its potency and selectivity make it a valuable tool for dissecting the roles of specific kinases in diverse biological contexts, providing insights into potential therapeutic strategies for diseases involving aberrant kinase activity.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 486.31 |
| Cas No. | 252935-94-7 |
| Formula | C20H17Cl2N9O2 |
| Synonyms | CT98014 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥8.1 mg/mL in DMSO with gentle warming |
| Chemical Name | 6-N-[2-[[4-(2,4-dichlorophenyl)-5-imidazol-1-ylpyrimidin-2-yl]amino]ethyl]-3-nitropyridine-2,6-diamine |
| SDF | Download SDF |
| Canonical SMILES | Nc(nc(cc1)NCCNc(nc2-c(ccc(Cl)c3)c3Cl)ncc2-[n]2cncc2)c1[N+]([O-])=O |
| 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. |
| Cell experiment: | |
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Cell lines |
Insulin receptor– expressing CHO-IR cells and primary rat hepatocytes |
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Preparation method |
The solubility of this compound in DMSO is <10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
24h; EC50=106 nM (CHO-IR cells); EC50=107 nM (rat hepatocytes). |
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Applications |
CHIR 98014 resulted in a stimulation of the GS activity ratio above basal. The concentrations of CHIR 98014 causing half-maximal GS stimulation (EC50) were 106 nM for CHO-IR cells and 107 nM for rat hepatocytes. |
| Animal experiment: | |
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Animal models |
Female db/db mice. |
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Dosage form |
30 mg/kg; oral taken |
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Applications |
Markedly diabetic and insulin-resistant db/db mice treated with 30 mg/kg CHIR 98014 exhibited a significant reduction in fasting hyperglycemia within 4 h of treatment and showed improved glucose disposal during an IPGTT. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Ring D B, Johnson K W, Henriksen E J, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo[J]. Diabetes, 2003, 52(3): 588-595. | |
| Description | CHIR-98014 is a potent inhibitor of GSK-3α and GSK-3β with IC50 values of 0.65 nM and 0.58 nM, respectively. | |||||
| Targets | GSK-3β | GSK-3α | p70 S6K | |||
| IC50 | 0.58 nM | 0.65 nM | >1 μM | |||
Quality Control & MSDS
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Chemical structure
