产品说明书
A-196
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同义名 : | - |
| CAS号 : | 1982372-88-2 | |
| 货号 : | A933282 | |
| 分子式 : | C18H16Cl2N4 | |
| 纯度 : | 99%+ | |
| 分子量 : | 359.252 | |
| MDL号 : | MFCD29924807 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 12 mg/mL(33.4 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The homologous protein lysine methyltransferases SUV420H1 and SUV420H2 (collectively named SUV4-20) are important regulators of genomic integrity. A-196 is a selective and potent SUV4-20 inhibitor. It inhibited the methyltransferase activity of SUV420H1 and SUV420H2 with IC50 values of 25 ± 5nM and 144 ± 21nM, respectively. A-196 also showed potent binding affinity for adenosine receptors A1 and A2A with Ki values of 0.021μM and 0.028μM, respectively. A-196 binds to SUV420H1 with a Kd value of 74.8 ± 22.7nM. Treatment of human osteosarcoma cell line U2OS with A-196 for 48 hours led to an increase in H4K20me1 level (EC50 = 735nM) and a decrease in both H4K20me2 (EC50 = 262nM) and H4K20me3 (EC50 = 370nM) levels. Also in U2OS cells, treatment with 6μM A-196 resulted in a robust increase in H4K20me1 level in the S phase and a decrease in H4K20me3 level. A-196 at 1 and 10μM inhibited the ability of primary B cells isolated from the spleens of wild-type mice to switch from IgM to IgG1, IgG3 or IgE[1]. | ||
| 作用机制 | A-196 inhibits SUV4-20 in a substrate-competitive manner. It binds within the histone H4 peptide-binding groove of the enzyme and is competitive with the histone peptide substrate, but not with the cofactor S-adenosylmethionine. There is strong cooperativity between the binding of A-196 and S-adenosylmethionine to SUV420H1[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.78mL 0.56mL 0.28mL |
13.92mL 2.78mL 1.39mL |
27.84mL 5.57mL 2.78mL |
| 参考文献 |
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