Molecular Formula | C13H12N6O2
|
Molar Mass | 284.27 |
Density | 1.531±0.06 g/cm3(Predicted) |
Boling Point | 534.9±50.0 °C(Predicted) |
Solubility | DMSO: ≥ 27 mg/mL |
Appearance | powder |
Color | yellow to orange |
pKa | 13.59±0.40(Predicted) |
Storage Condition | 2-8°C |
In vitro study | KRIBB11 inhibited the activity of HSF1 in a concentration-dependent manner. It can down regulate HSP70 and hsp27. KRIBB11 can inhibit the proliferation of cancer cells, arrest the cell cycle in G2/M phase and induce apoptosis. It has no inhibitory effect on the recruitment of HSF1 by the hsp70 promoter induced by heat shock, and has no inhibitory effect on the phosphorylation of the 230 Th serine of HSF1, however, inhibition of the heat shock-induced recruitment of the hsp70 promoter to pTEFb and p-TEFb phosphorylation of the polymerase II CTD at serine 2 is dependent. |
In vivo study | In mouse xenografts, KRIBB11 reduced tumor volume. In addition, the level of HSP70 protein was significantly decreased in tumors of mice treated with KRIBB11, indicating that KRIBB11 exerts its antitumor activity in vivo by inhibiting HSP70. |