产品说明书

SMI-16a

Print
Chemical Structure| 587852-28-6 同义名 : PIM1/2 Kinase Inhibitor VI
CAS号 : 587852-28-6
货号 : A310740
分子式 : C13H13NO3S
纯度 : 99%+
分子量 : 263.312
MDL号 : MFCD31382191
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(398.77 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：
生物活性
描述 Pim (provirus integration site for Moloney murine leukemia virus) family proteins are highly conserved serine/threonine kinases implicated in transcription, translation, cell cycle, survival, and drug resistance through the numerous targets. SMI-16a is a potent Pim kinase inhibitor with IC50 values of 0.15nM, 0.02nM and 48nM for Pim-1, Pim-2 and Pim-3 (measured by enzymatic activity), respectively[1]. Treatment with 5μM SMI-16a for 72h showed various degree of growth inhibition (10-40%) of PC3, DU145, LNCaP, U937, K562 and MV4;11 cells cultured in media containing 10% FBS. Because SMI-4a showed to be serum-bound, it was found that DU145 cells became considerably more sensitive under serum-free conditions. The translocation of p27Kip1 to the nucleus and reduced Cdk2 activity (shown by decreased p-H1) can also observed in K562 cells cultured in RPMI containing 10% FCS after treatment with SMI-16a[2]. Intraperitoneal injection of 50mg/kg of SMI-16a five days per week reduced tumor growth of female Balb/C mice injected subcutaneously with JC cells[1].
作用机制 SMI-16a can compete with respect to ATP, suggesting that it may bind within the ATP-binding pocket of the kinase.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.80mL

0.76mL

0.38mL

18.99mL

3.80mL

1.90mL

37.98mL

7.60mL

3.80mL
参考文献

[1]Xia Z, Knaak C, et al. Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases. J Med Chem. 2009 Jan 8;52(1):74-86.

[2]Beharry Z, Zemskova M, et al. Novel benzylidene-thiazolidine-2,4-diones inhibit Pim protein kinase activity and induce cell cycle arrest in leukemia and prostate cancer cells. Mol Cancer Ther. 2009 Jun;8(6):1473-83.