生物活性
CHIR-98014是一种非常有效的，选择性的，细胞可渗透的GSK-3抑制剂。
Targets
| Target | Value |
| GSK-3β | IC50: 0.58nM |
| GSK-3α | IC50: 0.65nM |
| p70S6K | IC50: >1μM |
| c-Src | IC50: >1μM |
| bFGFR | IC50: >1μM |
| KDR | IC50: >2μM |
| IGF-1R | IC50: >2μM |
| Insulin Receptor | IC50: >2μM |
| Cdc2 | IC50: 3.7μM |
| Akt1 | IC50: >5μM |
| Tie-2 | IC50: >5μM |
| FLT1 | IC50: >5μM |
| CK1ε | IC50: >5μM |
| ERK2 | IC50: >10μM |
| PKCα | IC50: >10μM |
| p90RSK2 | IC50: >10μM |
| Chk1 | IC50: >10μM |
| DNA-PK | IC50: >10μM |
| PI3K | IC50: >10μM |
化学数据
| 目录号 | A11085 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 486.3 |
| Formula | C20H17Cl2N9O2 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 252935-94-7 |
| Synonyms | CHIR98014 |
| SMILES | C1=CC(=C(C=C1Cl)Cl)C2=NC(=NC=C2N3C=CN=C3)NCCNC4=NC(=C(C=C4)[N+](=O)[O-])N |
溶解度
| In vitro (25°C) | DMSO | Warmed: 7 mg/mL (14.39 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 5% DMSO+corn oil | 1 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 20.56 mL | 102.82 mL | 205.63 mL |
| 0.5 mM | 4.11 mL | 20.56 mL | 41.13 mL |
| 1 mM | 2.06 mL | 10.28 mL | 20.56 mL |
| 5 mM | 0.41 mL | 2.06 mL | 4.11 mL |
*The above data is based on the productmolecular weight 486.3 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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