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

Name: SMI-16a
Brand: MedChemExpress
SKU: HY-101947
Rating: 5.0 (3 reviews)

Cat. No.: HY-101947 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 587852-28-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 108	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 108	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE SMI-16a

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PIM1 PIM2 PIM3

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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

PIM1

PIM2

Cellular Effect

Cell Line	Type	Value	Description	References
PC-12	IC₅₀	7 μM Compound: 9b	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	[PMID: 15109648]
PC-3	IC₅₀	48 μM Compound: 16a	Antiproliferative activity against human PC3 cells after 48 hrs by MTS assay Antiproliferative activity against human PC3 cells after 48 hrs by MTS assay	[PMID: 19072652]

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].

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

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].

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

Molecular Weight

263.31

Formula

C₁₃H₁₃NO₃S

CAS No.

587852-28-6

Appearance

Solid

Color

Light yellow to yellow

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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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.

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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 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

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.
Protocol 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

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (246 KB) HNMR (242 KB)

Handling Instructions (2659 KB)

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. [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]

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	[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

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

SMI-16a Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SMI-16a587852-28-6PIM1/2 Kinase Inhibitor VIPimPim kinasesInhibitorinhibitorinhibit

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

Customer Review

SMI-16a Related Antibodies

3 Publications Citing Use of MCE SMI-16a

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Pim Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

SMI-16a Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

SMI-16a Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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