1. JAK/STAT Signaling
    Apoptosis
  2. Pim
    Apoptosis
  3. TCS-PIM-1-4a

TCS-PIM-1-4a (Synonyms: SMI-4a)

Cat. No.: HY-16576 Purity: 99.73%
Handling Instructions

TCS-PIM-1-4a (SMI-4a) is a pan-Pim kinases inhibitor that blocks mTORC1 activity via activation of AMPK. TCS-PIM-1-4a kills a wide range of both myeloid and lymphoid cell lines (IC50 values ranging from 0.8 μM to 40 μM).

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TCS-PIM-1-4a Chemical Structure

TCS-PIM-1-4a Chemical Structure

CAS No. : 327033-36-3

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10 mM * 1  mL in DMSO USD 79 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

TCS-PIM-1-4a (SMI-4a) is a pan-Pim kinases inhibitor that blocks mTORC1 activity via activation of AMPK. TCS-PIM-1-4a kills a wide range of both myeloid and lymphoid cell lines (IC50 values ranging from 0.8 μM to 40 μM)[1][2].

IC50 & Target

Pim[1]

In Vitro

TCS-PIM-1-4a (10 μM; 24-48 hours; 6812/2 cells and Jurkat cells) treatment increases the population of cells in the G1 phase from 44.3% to 68.4% and from 56.2% to 67.1% in 6812/2 and Jurkat, respectively. S-phase cells are decreased in 6812/2, whereas only small changes are seen in Jurkat cells consistent with the lesser G1 block[1].
TCS-PIM-1-4a (5 μM; 6 hours; 6812/2 cells and Jurkat cells) induces cell death by the induction of apoptosis[1].
TCS-PIM-1-4a (5 μM; 4-8 hours; 6812/2 cells and Jurkat cells) prevents the increase in 4E-BP1 protein levels and inhibits mTOR-directed phosphorylation on Thr37/46[1].

Cell Cycle Analysis[1]

Cell Line: 6812/2 cells and Jurkat cells
Concentration: 10 μM
Incubation Time: 24 hours, 48 hours
Result: Induced cell-cycle arrest.

Apoptosis Analysis[1]

Cell Line: 6812/2 cells and Jurkat cells
Concentration: 5 μM
Incubation Time: 6 hours
Result: Led to an increase in the number of the cells positive for annexin V and negative for PI from 8.25% in the control to 21.85%.

Western Blot Analysis[1]

Cell Line: 6812/2 cells and Jurkat cells
Concentration: 10 μM
Incubation Time: 4 hours, 8 hours
Result: Prevented the increase in 4E-BP1 protein levels and inhibited mTOR-directed phosphorylation on Thr37/46.
In Vivo

TCS-PIM-1-4a (SMI-4a; 60 mg/kg; oral gavage; twice daily; for 21 days; nu/nu nude mice) treatment causes a significant delay in the tumor growth without any change in the weight, blood counts, or chemistries[1].

Animal Model: 18 Nu/nu nude mice with 6812/2 murine pre–T-LBL cells[1]
Dosage: 60 mg/kg
Administration: Oral gavage; twice daily; for 21 days
Result: Caused a significant delay in the tumor growth.
Molecular Weight

273.23

Formula

C₁₁H₆F₃NO₂S

CAS No.

327033-36-3

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)

*"≥" 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
10 mM 0.3660 mL 1.8300 mL 3.6599 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 (9.15 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.73%

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Keywords:

TCS-PIM-1-4aSMI-4aPimApoptosisPim kinasesLeukemiccell-cyclearrestp27Kip1apoptosisBakBax4E-BP1mTORC1Inhibitorinhibitorinhibit

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