1. Immunology/Inflammation Apoptosis
  2. SphK Apoptosis
  3. K145 hydrochloride

K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 μM and a Ki of 6.4 μM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity.

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K145 hydrochloride Chemical Structure

K145 hydrochloride Chemical Structure

CAS No. : 1449240-68-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
1 mg USD 44 In-stock
5 mg USD 110 In-stock
10 mg USD 170 In-stock
25 mg USD 310 In-stock
50 mg USD 466 In-stock
100 mg USD 700 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of K145 hydrochloride:

Top Publications Citing Use of Products

    K145 hydrochloride purchased from MedChemExpress. Usage Cited in: Am J Cancer Res. 2019 Mar 1;9(3):546-561.  [Abstract]

    Western immunoblotting analysis of NOXA protein levels in RBE and HCCC9810 cells treated with different concentrations of K145 for 24 h. Data shown represents 2 independent experiments.

    K145 hydrochloride purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2017 Nov 4;493(1):286-290.  [Abstract]

    Inhibition of pAkt by API-2 effectively prevents K145 induced increasing phosphorylation of FoxO1 in response to insulin. API-2 also significantly reverses K145 suppressed PEPCK and G6Pase mRNA and protein expression.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 μM and a Ki of 6.4 μM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity[1].

    IC50 & Target

    SphK2

     

    In Vitro

    K145 (0-10 μM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner[1].
    K145 (10 μM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells[1].
    K145 (4-8 μM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt[1].
    Treatment with K145 (10 μM) causes a decrease of total cellular S1P without significant effects on ceramide levels[1].

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

    Cell Viability Assay[1]

    Cell Line: U937 cells
    Concentration: 0 µM, 4 µM, 6 µM, 8 µM, 10 µM
    Incubation Time: 24 hours, 48 hours, 72 hours
    Result: Significantly inhibited the growth of U937 cells in a concentration-dependent manner.

    Apoptosis Analysis[1]

    Cell Line: U937 cells
    Concentration: 10 µM
    Incubation Time: 24 hours
    Result: Significantly induced apoptosis in U937 cells.

    Western Blot Analysis[1]

    Cell Line: U937 cells
    Concentration: 4 µM, 8 µM
    Incubation Time: 3 hours
    Result: Phosphorylated ERK and Akt were decreased.
    In Vivo

    K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice[1].

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

    Animal Model: BALB/c-nu mice injected with U937 cells[1]
    Dosage: 50 mg/kg
    Administration: Oral gavage; daily; for 15 days
    Result: Inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.
    Molecular Weight

    384.92

    Formula

    C18H25ClN2O3S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N(CCN)C/1=O)SC1=C/CCC2=CC=C(OCCCC)C=C2.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (129.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5979 mL 12.9897 mL 25.9794 mL
    5 mM 0.5196 mL 2.5979 mL 5.1959 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 (sealed storage, away from moisture). 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
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    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

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    Volume (final)

    V2

    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: ≥ 0.83 mg/mL (2.16 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (2.16 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.
    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.
    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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: 99.88%

    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 (sealed storage, away from moisture). 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 2.5979 mL 12.9897 mL 25.9794 mL 64.9486 mL
    5 mM 0.5196 mL 2.5979 mL 5.1959 mL 12.9897 mL
    10 mM 0.2598 mL 1.2990 mL 2.5979 mL 6.4949 mL
    15 mM 0.1732 mL 0.8660 mL 1.7320 mL 4.3299 mL
    20 mM 0.1299 mL 0.6495 mL 1.2990 mL 3.2474 mL
    25 mM 0.1039 mL 0.5196 mL 1.0392 mL 2.5979 mL
    30 mM 0.0866 mL 0.4330 mL 0.8660 mL 2.1650 mL
    40 mM 0.0649 mL 0.3247 mL 0.6495 mL 1.6237 mL
    50 mM 0.0520 mL 0.2598 mL 0.5196 mL 1.2990 mL
    60 mM 0.0433 mL 0.2165 mL 0.4330 mL 1.0825 mL
    80 mM 0.0325 mL 0.1624 mL 0.3247 mL 0.8119 mL
    100 mM 0.0260 mL 0.1299 mL 0.2598 mL 0.6495 mL
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    • 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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    Product Name:
    K145 hydrochloride
    Cat. No.:
    HY-15779A
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