产品说明书
C646
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同义名 : | - |
| CAS号 : | 328968-36-1 | |
| 货号 : | A122218 | |
| 分子式 : | C24H19N3O6 | |
| 纯度 : | 99%+ | |
| 分子量 : | 445.424 | |
| MDL号 : | MFCD01784780 | |
| 存储条件： |
粉末 Sealed in dry,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(26.94 mM)，配合低频超声，并水浴加热至45℃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： |
IP 2% DMSO+water 0.6 mg/mL clear PO 0.5% CMC-Na 13 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | The histone acetyltransferase p300/CBP is a transcriptional coactivator involved in many regulatory pathways during tumorigenesis. C646 is a selective and competitive p300 inhibitor with a Ki value of 400nM. Treatment of C3H 10T1/2 mouse fibroblasts with C646 (25μM) resulted in a reduction in the levels of histone H3 and H4 acetylation. C646 at a concentration of 25μM also inhibited TSA-induced acetylation in mouse fibroblasts. C646 at 10μM was capable of reducing 3H-thymidine incorporation in several human cancer cell lines. The IC50 value of C646 for the growth of melanoma cell line WM983A was 10-20μM[3] The suppression of P300 by C646 via intraperitoneal injection (30nmol/g/day for two weeks) reduced the level of blood glucose, rescued impaired autophagic flux, and resulted in an 18.5% increase in muscle mass in db/db mice.[4] | ||
| 作用机制 | C646 is a competitive, highly selective inhibitor of p300 versus other acetyltransferases.[3] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.25mL 0.45mL 0.22mL |
11.23mL 2.25mL 1.12mL |
22.45mL 4.49mL 2.25mL |
| 参考文献 |
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