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SMI-16a

Cat. No. M9274
SMI-16a Structure
Synonym:

PIM1/2 Kinase Inhibitor VI

Size Price Availability Quantity
10mM*1mL In DMSO USD 120 In stock
5mg USD 110 In stock
10mg USD 200 In stock
25mg USD 430 In stock
50mg USD 760 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro, treatment with Pim-2 short-interference RNA as well as the Pim inhibitor SMI-16a successfully restores osteoblastogenesis suppressed by all the above inhibitory factors and MM cells. The SMI-16a treatment potentiates BMP-2-mediated anabolic signaling while suppressing TGF-β signaling. 

In vivo, 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. SMI-16a does not have toxicity toward the liver as the albumin, alkaline phosphatase, and alanine aminotransferase levels are unchanged. SMI-16a effectively prevents bone destruction while suppressing MM tumor growth in MM animal models.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 263.31
Formula C13H13NO3S
CAS Number 587852-28-6
Purity >98%
Solubility DMSO: ≥ 60 mg/mL
Storage at -20°C
References

Pim-2 kinase is an important target of treatment for tumor progression and bone loss in myeloma.
Hiasa M, et al. Leukemia. 2015 Jan;29(1):207-17. PMID: 24787487.

Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases.
Xia Z, et al. J Med Chem. 2009 Jan 8;52(1):74-86. PMID: 19072652.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SMI-16a, PIM1/2 Kinase Inhibitor VI supplier, Pim, inhibitors

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