Kenpaullone is a potent inhibitor ofCDK1/cyclin BandGSK-3β, withIC₅₀s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 withIC₅₀s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor ofKLF4, reduces self-renewal of breastcancer stem cellsand cell motility in vitro.

Kenpaullone shows much less effect on c-src (IC₅₀, 15 μM), casein kinase 2 (IC₅₀, 20 μM), erk 1 (IC₅₀, 20 μM), and erk 2 (IC₅₀, 9 μM). Kenpaullone acts by competitive inhibition of ATP binding, and the apparent K_iis 2.5 μM. Kenpaullone can inhibit the growth of tumor cells in culture (mean GI₅₀, 43 μM) and causes altered cell cycle progression most clearly revealed under conditions of recovery from serum starvation^[1]. Kenpaullone demonstrates a wide range of biological utility, extending from maintenance of pancreatic β cell survival and proliferation to the induction of apoptosis in cancer cells^[2].

327.18

Solid

C₁₆H₁₁BrN₂O

142273-20-9

肯帕罗酮

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 35 mg/mL(106.97 mM)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制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

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (7.64 mM); Suspended solution

  此方案可获得 ≥ 2.5 mg/mL (7.64 mM，饱和度未知) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液