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Kenpaullone

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Chemical Structure| 142273-20-9 同义名 : NSC-664704;9-Bromopaullone;1-azakenpaullone
CAS号 : 142273-20-9
货号 : A196851
分子式 : C16H11BrN2O
纯度 : 98%
分子量 : 327.175
MDL号 : MFCD02683595
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(106.98 mM)，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
动物实验配方：

2% DMSO+50% PEG 300+5% Tween 80+water 2.5 mg/mL

生物活性
靶点

  • CDK5

    CDK5/p35, IC50:0.85μM

  • CDK2

    CDK2/CyclinE, IC50:7.5μM

    CDK2/CyclinA, IC50:0.68μM

  • CDK1

    CDK1/CyclinB, IC50:0.4μM
描述 (S) Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively[3]. Kenpaullone efficiently suppressed activity of glycogen synthase kinase (GSK) 3β. Combination therapy with kenpaullone and TMZ (temozolomide) suppressed stem cell phenotype and viability of both GSCs (glioma stem cell) and glioma cell lines. Combination therapy in mouse models significantly prolonged survival time compared with TMZ monotherapy[4]. KLF4 inhibitor Kenpaullone sensitizes breast cancer cells and xenograft tumors to Paclitaxel and improves therapeutic effects[5]. Moreover, kenpaullone plays a role in protecting cardiomyocytes from oxidative stress and that the turnover of Cx43 through SGSM3(small G protein signaling modulator 3)-induced lysosomal degradation underlies the anti-apoptotic effect of kenpaullone[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.06mL

0.61mL

0.31mL

15.28mL

3.06mL

1.53mL

30.56mL

6.11mL

3.06mL
参考文献

[1]Cole A, Frame S, Cohen P. Further evidence that the tyrosine phosphorylation of glycogen synthase kinase-3 (GSK3) in mammalian cells is an autophosphorylation event. Biochem J. 2004 Jan 1;377(Pt 1):249-55.

[2]Zaharevitz DW, Gussio R, et al. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res. 1999 Jun 1;59(11):2566-9.

[3]Zaharevitz DW, Gussio R, Leost M, Senderowicz AM, Lahusen T, Kunick C, Meijer L, Sausville EA. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res. 1999 Jun 1;59(11):2566-9

[4]Kitabayashi T, Dong Y, Furuta T, Sabit H, Jiapaer S, Zhang J, Zhang G, Hayashi Y, Kobayashi M, Domoto T, Minamoto T, Hirao A, Nakada M. Identification of GSK3β inhibitor kenpaullone as a temozolomide enhancer against glioblastoma. Sci Rep. 2019 Jul 11;9(1):10049

[5]Shi L, Tang X, Qian M, Liu Z, Meng F, Fu L, Wang Z, Zhu WG, Huang JD, Zhou Z, Liu B. A SIRT1-centered circuitry regulates breast cancer stemness and metastasis. Oncogene. 2018 Dec;37(49):6299-6315

[6]Joo HC, Choi JW, Moon H, Lee CY, Yoo KJ, Kim SW, Hwang KC. Protective effects of kenpaullone on cardiomyocytes following H2O2-induced oxidative stress are attributed to inhibition of connexin 43 degradation by SGSM3. Biochem Biophys Res Commun. 2018 May 5;499(2):368-373