1. JAK/STAT Signaling
  2. Pim
  3. SMI-4a

SMI-4a  (Synonyms: TCS-PIM-1-4a)

Cat. No.: HY-16576A Purity: 99.63%
SDS COA Handling Instructions

SMI-4a (TCS-PIM-1-4a) is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 μM. SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. SMI-4a has anticancer activity.

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

SMI-4a Chemical Structure

SMI-4a Chemical Structure

CAS No. : 438190-29-5

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of SMI-4a:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE SMI-4a

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  • Biological Activity

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Description

SMI-4a (TCS-PIM-1-4a) is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 μM. SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. SMI-4a has anticancer activity[1].

IC50 & Target[1]

PIM1

24 μM (IC50)

PIM1

0.6 μM (Ki)

PIM2

100 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
DLD-1 IC50
17.8 μM
Compound: 4
Inhibition of growth of DLD-1 cell line after 96 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of DLD-1 cell line after 96 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
DLD-1 IC50
31.4 μM
Compound: 4
Inhibition of growth of DLD-1 cell line after 72+72 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of DLD-1 cell line after 72+72 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
DLD-1 IC50
37.4 μM
Compound: 4
Inhibition of growth of DLD-1 cell line after 72 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of DLD-1 cell line after 72 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
DLD-1 IC50
40.1 μM
Compound: 4
Inhibition of growth of DLD-1 cell line after 24+72 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of DLD-1 cell line after 24+72 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
HCT-116 IC50
36.8 μM
Compound: 4
Inhibition of growth of HCT116 cell line after 72+72 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of HCT116 cell line after 72+72 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
HCT-116 IC50
45.5 μM
Compound: 4
Inhibition of growth of HCT116 cell line after 96 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of HCT116 cell line after 96 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
HCT-116 IC50
48.8 μM
Compound: 4
Inhibition of growth of HCT116 cell line after 72 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of HCT116 cell line after 72 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
HCT-116 IC50
91.7 μM
Compound: 4
Inhibition of growth of HCT116 cell line after 24+72 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of HCT116 cell line after 24+72 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
HCT-8 IC50
100 μM
Compound: 4
Inhibition of growth of HCT-8 cell line after 72 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of HCT-8 cell line after 72 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
HCT-8 IC50
82.2 μM
Compound: 4
Inhibition of growth of HCT-8 cell line after 96 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of HCT-8 cell line after 96 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
HL-60 GI50
4.9 μM
Compound: SMI-4a
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
[PMID: 34958208]
HT-29 IC50
31.4 μM
Compound: 4
Inhibition of growth of HT-29 cell line after 72+72 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of HT-29 cell line after 72+72 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
HT-29 IC50
38.8 μM
Compound: 4
Inhibition of growth of HT-29 cell line after 72 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of HT-29 cell line after 72 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
HT-29 IC50
59.7 μM
Compound: 4
Inhibition of growth of HT-29 cell line after 96 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of HT-29 cell line after 96 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
HT-29 IC50
71.7 μM
Compound: 4
Inhibition of growth of HT-29 cell line after 24+72 hours of exposure time with the compound dissolved in DMSO
Inhibition of growth of HT-29 cell line after 24+72 hours of exposure time with the compound dissolved in DMSO
[PMID: 15993594]
MOLM-13 GI50
2.16 μM
Compound: SMI-4a
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
[PMID: 34958208]
Mononuclear cell line GI50
8.35 μM
Compound: SMI-4a
Antiproliferative activity against AML patient derived mononuclear cells of assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against AML patient derived mononuclear cells of assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
[PMID: 34958208]
PC-3 IC50
17 μM
Compound: 4a
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-4a (0.5 μM; 1 hour; HEK-293T cells) treatment attenuates the autophosphorylation of tagged Pim-1 in intact cells[1].

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

Western Blot Analysis[1]

Cell Line: HEK-293T cells
Concentration: 0.5 µM
Incubation Time: 1 hour
Result: Caused a dose-dependent reduction in Pim-1-induced 4E-BP1 phosphorylation, with an IC50 of approximately 125 nM.
Molecular Weight

273.23

Formula

C11H6F3NO2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC/1=O)SC1=C/C2=CC=CC(C(F)(F)F)=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 (365.99 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 3.6599 mL 18.2996 mL 36.5992 mL
5 mM 0.7320 mL 3.6599 mL 7.3198 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  0.5% CMC-Na/saline water

    Solubility: 2 mg/mL (7.32 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  20% HP-β-CD in Saline

    Solubility: 5 mg/mL (18.30 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.63%

References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6599 mL 18.2996 mL 36.5992 mL 91.4980 mL
5 mM 0.7320 mL 3.6599 mL 7.3198 mL 18.2996 mL
10 mM 0.3660 mL 1.8300 mL 3.6599 mL 9.1498 mL
15 mM 0.2440 mL 1.2200 mL 2.4399 mL 6.0999 mL
20 mM 0.1830 mL 0.9150 mL 1.8300 mL 4.5749 mL
25 mM 0.1464 mL 0.7320 mL 1.4640 mL 3.6599 mL
30 mM 0.1220 mL 0.6100 mL 1.2200 mL 3.0499 mL
40 mM 0.0915 mL 0.4575 mL 0.9150 mL 2.2875 mL
50 mM 0.0732 mL 0.3660 mL 0.7320 mL 1.8300 mL
60 mM 0.0610 mL 0.3050 mL 0.6100 mL 1.5250 mL
80 mM 0.0457 mL 0.2287 mL 0.4575 mL 1.1437 mL
100 mM 0.0366 mL 0.1830 mL 0.3660 mL 0.9150 mL
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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.

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