SMI-16a
Based on 6 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.0%
- CAS. Nr.: 587852-28-6
- Formel: C13H13NO3S
- Molecular Weight:263.31
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) SMI-16a
More
Biologische Aktivität
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PIM1 |
PIM2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PC-12 | IC50 |
7 μM
Compound: 9b
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Concentration required for 50% inhibition of cell proliferation in PC12 cells using sulforhodamine B assay
Concentration required for 50% inhibition of cell proliferation in PC12 cells using sulforhodamine B assay
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[PMID: 15109648] |
| PC-3 | IC50 |
48 μM
Compound: 16a
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Antiproliferative activity against human PC3 cells after 48 hrs by MTS assay
Antiproliferative activity against human PC3 cells after 48 hrs by MTS assay
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[PMID: 19072652] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 587852-28-6
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Appearance Solid
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Molecular Weight 263.31
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Formel C13H13NO3S
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Color Light yellow to yellow
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SMILES
O=C(NC/1=O)SC1=C\C2=CC=C(OCCC)C=C2
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Synonyms
PIM1/2 Kinase Inhibitor VI
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Combining PIM-2 and PARP1 Inhibitors Induces MICA Expression on Multiple Myeloma Cells to Activate NK Cells through NKG2D Binding. [Abstract]2025 Jun 25:e02448. PMID: 40557764 -
Cancers (Basel)
2022 Dec 22;15(1):67. PMID: 36612063 -
bioRxiv
HIV-associated non-Hodgkin lymphoma tumor-microenvironment axes differ by EBV status across cellular origins. [Abstract]2025 Oct 16:2025.10.15.682084. PMID: 41279969 -
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Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (379.78 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7978 mL | 18.9890 mL | 37.9780 mL | 94.9451 mL |
| 5 mM | 0.7596 mL | 3.7978 mL | 7.5956 mL | 18.9890 mL | |
| 10 mM | 0.3798 mL | 1.8989 mL | 3.7978 mL | 9.4945 mL | |
| 15 mM | 0.2532 mL | 1.2659 mL | 2.5319 mL | 6.3297 mL | |
| 20 mM | 0.1899 mL | 0.9495 mL | 1.8989 mL | 4.7473 mL | |
| 25 mM | 0.1519 mL | 0.7596 mL | 1.5191 mL | 3.7978 mL | |
| 30 mM | 0.1266 mL | 0.6330 mL | 1.2659 mL | 3.1648 mL | |
| 40 mM | 0.0949 mL | 0.4747 mL | 0.9495 mL | 2.3736 mL | |
| 50 mM | 0.0760 mL | 0.3798 mL | 0.7596 mL | 1.8989 mL | |
| 60 mM | 0.0633 mL | 0.3165 mL | 0.6330 mL | 1.5824 mL | |
| 80 mM | 0.0475 mL | 0.2374 mL | 0.4747 mL | 1.1868 mL | |
| 100 mM | 0.0380 mL | 0.1899 mL | 0.3798 mL | 0.9495 mL |
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