产品说明书
MS436
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同义名 : | - |
| CAS号 : | 1395084-25-9 | |
| 货号 : | A113750 | |
| 分子式 : | C18H17N5O3S | |
| 纯度 : | 99%+ | |
| 分子量 : | 383.424 | |
| MDL号 : | MFCD27992062 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 25 mg/mL(65.2 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： |
| 生物活性 | |||
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| 靶点 |
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| 描述 | BRD4 is a key chromatin organizer characterized by two acetyl-lysine binding bromodomains and an extra-terminal domain. It contains two tandem bromodomains, BrD1 and BrD2. MS436 is a bromodomain inhibitor that shows potent affinity for BRD4 BrD1 with an estimated Ki value of 30-50nM and a 10-fold selectivity for BrD1 over BrD2. It also exhibits inhibitory activities against BRD3 BrD1, BRD3 BrD2, CBP, PCAF, BRD7, BPTF, BAZ2b, and SMARCA4 with Ki values of 0.10, 0.14, 2.18, 5.52, 2.72, 6.06, 3.29, and 7.97µM, respectively. MS436 displayed excellent physiochemical properties with ligand efficiency, CLogP, and lipophilic ligand efficiency of 12.66, 2.65, and 3.42, respectively. In murine macrophage RAW264.7 cells, MS436 effectively inhibited BRD4 activity in NF-κB-directed production of nitric oxide and interleukin-6 with IC50 values of 4.9 and 3.8µM, respectively[2]. | ||
| 作用机制 | MS436 is a low nanomolar, small-molecule bromodomain inhibitor that inhibits BRD4 through a set of water-mediated interactions. Besides five water molecules stably located at the bottom of the acetyl-lysine binding pocket in bromodomains, more bound water molecules were observed engaging in the ligand recognition with MS436[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.61mL 0.52mL 0.26mL |
13.04mL 2.61mL 1.30mL |
26.08mL 5.22mL 2.61mL |
| 参考文献 |
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