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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] |
Dose | Mice (i.p.): 5 mg/kg[2], 50 mg/kg[3], 65 mg/kg[4] |
Administration | i.p. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.52mL 0.70mL 0.35mL |
17.59mL 3.52mL 1.76mL |
35.18mL 7.04mL 3.52mL |
CAS号 | 342639-96-7 |
分子式 | C13H12N6O2 |
分子量 | 284.27 |
SMILES Code | O=[N+](C1=CC=C(NC)N=C1NC2=CC3=C(NN=C3)C=C2)[O-] |
MDL No. | MFCD30182306 |
别名 | |
运输 | 蓝冰 |
InChI Key | NDJJEQIMIJJCLL-UHFFFAOYSA-N |
Pubchem ID | 69894253 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
溶解方案 |
DMSO: 120 mg/mL(422.13 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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