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

TCS PIM-1 1 (Synonyms: SC 204330)

Cat. No.: HY-18086 Purity: 98.03%
Handling Instructions

TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM).

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

TCS PIM-1 1 Chemical Structure

TCS PIM-1 1 Chemical Structure

CAS No. : 491871-58-0

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 143 In-stock
Estimated Time of Arrival: December 31
10 mg USD 130 In-stock
Estimated Time of Arrival: December 31
50 mg USD 564 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    TCS PIM-1 1 purchased from MCE. Usage Cited in: J Cent South Univ. 2018, 43(5): 481-489.

    Effect of Pim-1 inhibitor on expression of T cell transcription factors in mice (n=5) A: Control group; B: TNBS group; C: TNBS+small doses of Pim-1 inhibitor group; D: TNBS+high doses of Pim-1 inhibitor group; E: TNBS+prednisone group.
    • Biological Activity

    • Purity & Documentation

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    • Customer Review

    Description

    TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM)[1].

    IC50 & Target[1]

    PIM1

    50 nM (IC50)

    In Vitro

    TCS PIM-1 1 (compound 1), a substituted pyridone scaffold, binds convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggests that TCS PIM-1 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2. Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors. TCS PIM-1 1 serves both as a starting point for SAR chemical syntheses and was used for co-crystallization with Pim-1 protein[1].

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

    Molecular Weight

    367.20

    Formula

    C₁₈H₁₁BrN₂O₂

    CAS No.

    491871-58-0

    SMILES

    OC1=C(C(N2)=CC(C3=CC=CC=C3)=C(C#N)C2=O)C=C(Br)C=C1

    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 (272.33 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7233 mL 13.6166 mL 27.2331 mL
    5 mM 0.5447 mL 2.7233 mL 5.4466 mL
    10 mM 0.2723 mL 1.3617 mL 2.7233 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      TCS PIM-1 1 is dissolved in 0.5% DMSO[2].

    References
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    Keywords:

    TCS PIM-1 1SC 204330SC204330SC-204330PimPim kinasesPim-1pyridonescaffoldATP-competitiveInhibitorinhibitorinhibit

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    Product Name:
    TCS PIM-1 1
    Cat. No.:
    HY-18086
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