1. JAK/STAT Signaling
  2. Pim
  3. SMI-16a

SMI-16a (Synonyms: PIM1/2 Kinase Inhibitor VI)

Cat. No.: HY-101947 Purity: 99.70%
Handling Instructions

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.

For research use only. We do not sell to patients.

SMI-16a Chemical Structure

SMI-16a Chemical Structure

CAS No. : 587852-28-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
25 mg USD 468 In-stock
Estimated Time of Arrival: December 31
50 mg USD 828 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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.

IC50 & Target

IC50: 0.15 μM (Pim1), 0.02 μM (Pim2), 48 μM (PC3 cells)[1]

In Vitro

SMI-16a has excellent potency for inhibition of both Pim-1 and Pim-2[1]. 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[2].

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].

Molecular Weight

263.31

Formula

C₁₃H₁₃NO₃S

CAS No.

587852-28-6

SMILES

O=C(NC/1=O)SC1=C\C2=CC=C(OCCC)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (379.78 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7978 mL 18.9890 mL 37.9781 mL
5 mM 0.7596 mL 3.7978 mL 7.5956 mL
10 mM 0.3798 mL 1.8989 mL 3.7978 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.49 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.49 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.49 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Recombinant human Pim-1 (Upstate) is incubated with S6 kinase/Rsk-2 peptide 2 (KKRNRTLTK) as the substrate in the presence 100 µM of compounds from the screening library, 1 µM ATP and 10 mM MgCl2 for 1 h. The Kinase-Glo luciferase kit is used to measure residual ATP levels after the kinase reaction[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Human prostate cancer PC3 cells are seeded in 96-well tissue culture dishes at approximately 10% confluency and allowed to attach and recover for 24 h. Varying concentrations of the test compounds (SMI-16a) are then added to each well, and the plates are incubated for an additional 48 h. The number of surviving cells is determined by the MTS assay. The percentage of cells killed is calculated as the percentage decrease in MTS metabolism compared with control cultures[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Female Balb/C mice are injected subcutaneously with JC cells suspended in PBS. After palpable tumor growth, animals are treated five days per week by intraperitoneal injection of vehicle alone or 50 mg/kg of SMI-16a.Whole body weights and tumor volume measurements are performed three times per week[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

SMI-16aPIM1/2 Kinase Inhibitor VIPimPim kinasesInhibitorinhibitorinhibit

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