In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SMI-4a is a selective inhibitor of Pim1 with IC50 value of 17 nM  .
Pim-1 is an enzyme that is encoded by human PIM1 gene and it has been revealed that Pim-1 directly involved in the regulation of cell cycle progression and apoptosis and many studies have shown that Pim were over-expressed and promote cell growth and survival in a veraity of solid cancers and hematologic malignancies [3, 4].
SMI-4a is a selective Pim inhibitor and more active than the reported SMI-16a. When tested with human erythroleukemia cell line K562 cells, SIM-4a treatment modulated cell growth and activated AMPK which inhibited mTORC1 activity by inhibiting Pim activity . In 25 leukemic cell lines, administration of SMI-4a induced cell-cycle arrest, elevated cell apoptosis, and pre–T-LBL/T-ALL being the highly sensitive cell line through mitochondrial pathway and inhibition of the mTORC1 pathway .
In Nu/nu nude mice model with 2 × 106 6812/2 cells subcutaneous xenograft, oral administration of SMI-4a from the third day for 5 of 7 days per week until day 21 on twice daily schedule significantly reduced tumor sizse .
. Beharry, Z., 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. 8(6): p. 1473-83.
. Lin, Y.W., et al., A small molecule inhibitor of Pim protein kinases blocks the growth of precursor T-cell lymphoblastic leukemia/lymphoma. Blood, 2010. 115(4): p. 824-33.
. Liu, Z., et al., Computational prediction and experimental validation of a novel synthesized pan-PIM inhibitor PI003 and its apoptosis-inducing mechanisms in cervical cancer. Oncotarget, 2015.
. Warfel, N.A. and A.S. Kraft, PIM kinase (and Akt) biology and signaling in tumors. Pharmacol Ther, 2015.
. Beharry, Z., et al., The Pim protein kinases regulate energy metabolism and cell growth. Proc Natl Acad Sci U S A, 2011. 108(2): p. 528-33.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||insoluble in H2O; ≥13.65 mg/mL in DMSO; ≥47.1 mg/mL in EtOH|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.|
|Description||SMI-4a is an inhibitor of Pim kinase.|