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

TCS PIM-1 1  (Synonyms: SC 204330)

Cat. No.: HY-18086 Purity: 98.01%
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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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 143 In-stock
Solution
10 mM * 1 mL in DMSO USD 143 In-stock
Solid
5 mg USD 83 In-stock
10 mg USD 130 In-stock
25 mg USD 245 In-stock
50 mg USD 363 In-stock
100 mg USD 540 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

TCS PIM-1 1 Related Antibodies

Top Publications Citing Use of Products

    TCS PIM-1 1 purchased from MedChemExpress. 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.

    View All Pim Isoform Specific Products:

    View All Isoforms
    PIM1 PIM2 PIM3

    • Biological Activity

    • Purity & Documentation

    • References

    • 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].

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

    TCS PIM-1 1 Related Antibodies
    Molecular Weight

    367.20

    Formula

    C18H11BrN2O2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (272.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    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)

    Mass
    =
    Concentration
    ×
    Volume
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    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:

    The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

    • Protocol 1

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

    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
    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, 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 2.7233 mL 13.6166 mL 27.2331 mL 68.0828 mL
    5 mM 0.5447 mL 2.7233 mL 5.4466 mL 13.6166 mL
    10 mM 0.2723 mL 1.3617 mL 2.7233 mL 6.8083 mL
    15 mM 0.1816 mL 0.9078 mL 1.8155 mL 4.5389 mL
    20 mM 0.1362 mL 0.6808 mL 1.3617 mL 3.4041 mL
    25 mM 0.1089 mL 0.5447 mL 1.0893 mL 2.7233 mL
    30 mM 0.0908 mL 0.4539 mL 0.9078 mL 2.2694 mL
    40 mM 0.0681 mL 0.3404 mL 0.6808 mL 1.7021 mL
    50 mM 0.0545 mL 0.2723 mL 0.5447 mL 1.3617 mL
    60 mM 0.0454 mL 0.2269 mL 0.4539 mL 1.1347 mL
    80 mM 0.0340 mL 0.1702 mL 0.3404 mL 0.8510 mL
    100 mM 0.0272 mL 0.1362 mL 0.2723 mL 0.6808 mL
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    TCS PIM-1 1 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:

    TCS PIM-1 1491871-58-0SC 204330SC204330SC-204330PimPim kinasesPim-1pyridonescaffoldATP-competitiveInhibitorinhibitorinhibit

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