CHIR-98014
Based on 11 publication(s) in Google Scholar
CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor with IC50s of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively; it shows less potent activities against cdc2 and erk2.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.44%
- CAS 番号: 252935-94-7
- 分子式: C20H17Cl2N9O2
- 分子量:486.31
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 CHIR-98014
More- Cell Res. 2022 Jun;32(6):513-529. [Abstract]
- Cancer Res. 2019 Feb 1;79(3):534-545. [Abstract]
- Adv Sci (Weinh). 2026 Apr;13(23):e11606. [Abstract]
- Sci Adv. 2026 Mar 20;12(12):eadz5906. [Abstract]
- Neuro Oncol. 2026 Jul 23:noag167.
- SLAS Discov. 2024 Nov 5;29(8):100191. [Abstract]
- Food Chem Toxicol. 2025 Oct:204:115628. [Abstract]
- Hum Cell. 2024 Jul;37(4):1156-1169. [Abstract]
- SSRN. 2025 Jul 25.
- bioRxiv. 2024 September 07.
- SSRN. 2023 Jun 20.
生物活性
製品説明
IC50 & Target
[1]|
GSK-3β 0.58 nM (IC50) |
GSK-3α 0.65 nM (IC50) |
cdc2 3700 nM (IC50) |
体外実験
CHIR 98014 inhibits human GSK-3β with Ki value of 0.87 nM. CHIR 98014 causes GS stimulation in CHO-IR cells and rat hepatocytes, with EC50s of 106 nM and 107 nM, respectively[1]. CHIR-98014 (1 μM) reduces the viability of ES-CCE cells by 52%, with IC50 of 1.1 μM. Moreover, CHIR-98014 in combination with CHIR-99021 results in a significant activation of the Wnt/beta-catenin pathway in ES-D3 cells. In CHIR-98014 treated cells, the T gene expression is induced up to 2,500-fold. CHIR-98014 (1 μM) also yields around 50% Brachyury-positive cells, with EC50 of 0.32 μM[2]. CHIR98014 (10 μM) prevents loss of neurites caused by 20 μM PrP1-30 in cortical and hippocampal neurons, and substantially decreases the amount of dead cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 252935-94-7
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性状 Solid
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分子量 486.31
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分子式 C20H17Cl2N9O2
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Color Light yellow to yellow
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SMILES
ClC1=CC(Cl)=CC=C1C2=NC(NCCNC3=CC=C([N+]([O-])=O)C(N)=N3)=NC=C2N4C=CN=C4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (11)
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Journal Impact Factor
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Most Recent
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Cell Res
Derivation of totipotent-like stem cells with blastocyst-like structure forming potential. [Abstract]2022 Jun;32(6):513-529. PMID: 35508506 -
Cancer Res
A GYS2/p53 Negative Feedback Loop Restricts Tumor Growth in HBV-Related Hepatocellular Carcinoma. [Abstract]2019 Feb 1;79(3):534-545. PMID: 30584071 -
Adv Sci (Weinh)
PDZK1-ULK1 Axis Triggers Lipophagy to Inhibit Tumor Progression and Sunitinib Resistance in Clear Cell Renal Cell Carcinoma. [Abstract]2026 Apr;13(23):e11606. PMID: 41698049 -
Sci Adv
Caspase-3/7 deficiency results in enhanced intestinal inflammation and reduced tumorigenesis. [Abstract]2026 Mar 20;12(12):eadz5906. PMID: 41861024 -
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SLAS Discov
Development of a live cell assay for real-time monitoring the interactions between the Hippo pathway components 14-3-3 and TAZ. [Abstract]2024 Nov 5;29(8):100191. PMID: 39510350 -
Food Chem Toxicol
Mechanistic insights into AKT1/GSK3β/CD36 axis regulation in ZLY06-induced hepatic lipid metabolism dysfunction and protective intervention via AKT activation strategies. [Abstract]2025 Oct:204:115628. PMID: 40633829 -
Hum Cell
β-Sitosterol alleviates the malignant phenotype of hepatocellular carcinoma cells via inhibiting GSK3B expression. [Abstract]2024 Jul;37(4):1156-1169. PMID: 38814517 -
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溶剤 & 溶解度
体外:
DMSO : 12.5 mg/mL (25.70 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95. [Content Brief]
[2]. Naujok O, et al. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors. BMC Res Notes. 2014 Apr 29;7:273. [Content Brief]
[3]. Zajkowski T, et al. Stabilization of microtubular cytoskeleton protects neurons from toxicity of N-terminal fragment of cytosolic prion protein. Biochim Biophys Acta. 2015 Oct;1853(10 Pt A):2228-39. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0563 mL | 10.2815 mL | 20.5630 mL | 51.4075 mL |
| 5 mM | 0.4113 mL | 2.0563 mL | 4.1126 mL | 10.2815 mL | |
| 10 mM | 0.2056 mL | 1.0282 mL | 2.0563 mL | 5.1408 mL | |
| 15 mM | 0.1371 mL | 0.6854 mL | 1.3709 mL | 3.4272 mL | |
| 20 mM | 0.1028 mL | 0.5141 mL | 1.0282 mL | 2.5704 mL | |
| 25 mM | 0.0823 mL | 0.4113 mL | 0.8225 mL | 2.0563 mL |