KRIBB11
产品说明书
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同义名 : | - |
| CAS号 : | 342639-96-7 | |
| 货号 : | A114945 | |
| 分子式 : | C13H12N6O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 284.27 | |
| MDL号 : | MFCD30182306 | |
| 存储条件： |
Pure form Keep in dark place, sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | HSF1 (heat shock factor 1) is the master switch for heat shock protein (HSP) expression in eukaryotes. KRIBB11 is an HSF1 inhibitor with IC50 value of 1.2 μM for abolishing the heat shock-induced luciferase activity. Exposure to KRIBB11 at concentration < 50 μM 30min prior to heat shock at 43℃ for 1 h and further incubation at 37℃ for 1 h could dose-dependently inhibit the heat shock-induced transcription of hsp70, hsp47, and hsp27 in HCT116 cells. And this concentration-dependent inhibition of hsp70 and hsp27 can be also observed on protein level at concentration < 10 μM. Treatment with KRIBB11 for 48h at concentration ranging in 1-30 μM could inhibit proliferation of HCT116 cells by arresting the cell cycle at the G2/M phase, and apoptosis can be induced in both dose (1-20 μM, for 48 h)- and time (10 μM, 3-48 h)-dependent manner. Intraperitoneal injection with KRIBB11 at 50 mg/kg for 18 days could inhibit tumor growth in HCT-116 cells xenograft mice, with much lower expression of HSP70 observed in tumor tissue[1]. | ||
| 作用机制 | KRIBB11 can bind to HSF-1 and inhibit heat shock-induced recruitment of p-TEFb to the hsp70 promoter and phosphorylation of RNA pol II CTD Ser-2.[1] | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.52mL 0.70mL 0.35mL |
17.59mL 3.52mL 1.76mL |
35.18mL 7.04mL 3.52mL |
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