SMI-16a
SMI-16a Basic information
- Product Name:
- SMI-16a
- Synonyms:
-
- SMI-16a
- PIM1/2 Kinase Inhibitor VI
- SMI-16a(PIM1/2 Kinase Inhibitor VI)
- SMI-16A;SMI 16A;SMI16A
- 2,4-Thiazolidinedione, 5-[(4-propoxyphenyl)methylene]-
- SMI-16a,SMI 16a,inhibit,SMI16a,Pim,Inhibitor,Pim kinases
- 5-(4-propoxybenzylidene)thiazolidine-2,4-dione
- SMI-16a, 10 mM in DMSO
- CAS:
- 587852-28-6
- MF:
- C13H13NO3S
- MW:
- 263.31
- Mol File:
- 587852-28-6.mol
SMI-16a Chemical Properties
- Melting point:
- 186.3-188.4 °C
- Density
- 1.303±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C(protect from light)
- solubility
- Ethanol:3.0(Max Conc. mg/mL);11.39(Max Conc. mM)
- form
- A solid
- pka
- 7.27±0.20(Predicted)
- color
- Light yellow to yellow
SMI-16a Usage And Synthesis
Description
SMI-16a is a Pim-1 kinase inhibitor (IC50 = 63 nM). It is selective for Pim-1 over a panel of 60 kinases. SMI-16a (5 μM) inhibits phosphorylation of the Pim-1 target protein Bad in DU145-Pim cells and inhibits the growth of PC3, DU145, LNCaP, K562, and MV4-11 cancer cells. It induces apoptosis and cell cycle arrest at the G1 phase in DU145 cells.
Uses
SMI-16a is a selective Pim kinase inhibitor with IC50 values of 0.15, 0.02 and 48 μM for Pim1, Pim2 and PC3 cells, respectively.
in vivo
Mice tolerate intraperitoneal dose of SMI-16a is 50 mg/kg daily for 5 days, while 100 mg/kg is overtly toxic. Treatment of the animals with SMI-16a for 5 days per week reduces the growth of tumors by approximately 50% and does not cause a loss of body weight. Subchronic dosing with SMI-16a does not affect the levels of red, white blood cells, including lymphocytes, monocytes, and granulocytes, indicating that the compound does not have myelosuppressive effects. SMI-16a does not have toxicity toward the liver as the albumin, alkaline phosphatase, and alanine aminotransferase levels are unchanged [1]. SMI-16a effectively prevents bone destruction while suppressing MM tumor growth in MM animal models[2].
IC 50
PIM1; PIM2
References
[1] Xia Z, 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. DOI:10.1021/jm800937p
[2] Hiasa M, et al. Pim-2 kinase is an important target of treatment for tumor progression and bone loss in myeloma. Leukemia. 2015 Jan;29(1):207-17. DOI:10.1038/leu.2014.147
SMI-16aSupplier
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