1. IC261

IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.

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

IC261 Chemical Structure

IC261 Chemical Structure

CAS No. : 186611-52-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 88 In-stock
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Solid
5 mg USD 80 In-stock
10 mg USD 130 In-stock
25 mg USD 230 In-stock
50 mg USD 350 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    IC261 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2020 Jan 17;16(5):882-892.  [Abstract]

    The expression of cleaved caspase-3 of RKO and HCT116 induced by IC261 is detected by using Western blotting (*p<0.05, **p<0.01 vs 0 nM group).
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • Customer Review

    Description

    IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.

    IC50 & Target

    IC50: 1 μM (Ckiδ), 1 μM (Ckiε), 16 μM (Ckiα1)[1]

    In Vitro

    IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively. IC261 is less active on PKA, p34cdc2, and p55fyn (IC50s > 100 μM)[1]. IC261 induces mitotic arrest, spindle defects and centrosome amplification in AC1-M88 cells. IC261 (1 μM) increases G2/M cells after 12 h, and causes cell death at 24 h in AC1-M88 cells. IC261 (1 μM) also induces apoptosis in the extravillous trophoblast hybrid cells[2]. IC261 (1.25 μM) suppresses the proliferation of several pancreatic tumour cell lines, including ASPC-1, BxPc3, Capan-1, Colo357, MiaPaCa-2, Panc1, Panc89, PancTu-1 and PancTu-2 cells. IC261 (1.25 μM) specifically enhances CD95-mediated apoptosis of pancreatic tumour cells[3].

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

    In Vivo

    IC261 (20.5 mg/kg) inhibits tumor growth of PancTu-2 cells in SCID mice, downregulates several anti-apoptotic proteins, such as CK1δ/∊, KRAS, and IL6 and upregulates p21, ATM, CHEK1 and STAT1 in mice[3].

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

    Molecular Weight

    311.33

    Formula

    C18H17NO4

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to khaki

    SMILES

    O=C1NC2=C(C=CC=C2)/C1=C\C3=C(OC)C=C(OC)C=C3OC

    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 (321.20 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 3.2120 mL 16.0601 mL 32.1203 mL
    5 mM 0.6424 mL 3.2120 mL 6.4241 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 2.5 mg/mL (8.03 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    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:
    %
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    %
    Tween-80 +
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    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).
    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
    Kinase Assay
    [1]

    Casein kinase activity is assayed at 37°C. The standard reaction (40 μL) contains 25 mM 2-(N-morpholino)ethanesulfonic acid, pH 6.5, 50 mM NaCl, 15 mM MgCl2, 2 mg/mL casein, 2 mM EGTA, 100 μM [γ-32P]ATP (100-400 cpm/pmol). Initial velocity measurements are carried out in duplicate with ATP as the varied substrate. Kinetic constants and their standard errors are calculated. For assay of inhibitor potency (IC50), [γ -32P]ATP is held constant (10 μM), whereas IC261 concentration is varied (0.1, 0.3, 1, 3, and 10 μM). To assess kinetic mechanism, inhibitors are held constant (IC261, 20 μM; IC3608, 100 μM), whereas [γ -32P]ATP is varied as above. For screening small molecule libraries, CK1 isoforms (Ckiα1, δ, and ε) are assayed that casein is used at 10 mg/mL, [γ -32P]ATP is held constant at 2 μM or 1 mM[1].

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

    Cell Assay
    [2]

    Human extravillous trophoblast cells irreversibly leave the cell cycle and die when isolated from its natural extracellular matrix. The cell line AC1-M88 is employed in vitro experiments. This cell line is generated by fusion of extravillous trophoblasts with AC1-1. Cells are grown in DMEM (CV-1) or DMEM/F-12 (AC1-M88) medium supplemented with 10% fetal calf serum (FCS) at 37°C in a humidified 5% CO2 atmosphere. Where indicated, cells are γ-irradiated with 5 Gy and harvested at the given time points for western blot analysis, treated with 1 μM IC261 or 0.4 μM nocodazole for 12 h and fixed for immunofluorescence analysis, or treated with 1 μM IC261 and fixed for flow cytometrical analysis or lysed for western blot analysis at the indicated time points. IC261 and nocodazole are dissolved in DMSO as stock solutions (25 and 10 mM, respectively), and control cells are treated with 0.004% DMSO. For immunocytochemistry, the cells are grown on coverslips and are treated with methanol (−20°C) for 5 min, followed by acetone (−20°C) for 20-30 s prior to being used for immunocytochemical detection[2].

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

    Animal Administration
    [3]

    Five million PancTu-1 cells resuspended in 100 µL of a solution containing 50% Matrigel and 50% DMEM/RPMI-1640 (1:1) are injected into the dorsolateral site of 6-week-old C.B-17/IcrHsd-scid-bg mice. After 17 days, mice are randomised to the control group (n = 5), the IC261 treatment group (n = 5), the gemcitabine group (n = 5) and to the IC261/gemcitabine group (n = 5). Injection of dimethylsulfoxide (DMSO; control group), IC261 (20.5 mg/kg), gemcitabine (0.6 mg/kg) alone or in combination (20.5 mg/kg IC261/0.6 mg/kg gemcitabine) (treatment groups) is performed daily for 8 days. Mice are sacrificed by asphyxiation with CO2 the day after the last treatment. Tumours are measured before and during treatment. Finally, the tumours are excised, measured, weighed and fixed in formalin or shock frozen. Tumour volume is calculated according to the formula for a rotational ellipsoid (length × height × width × 0.5236)[3].

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

    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 3.2120 mL 16.0601 mL 32.1203 mL 80.3006 mL
    5 mM 0.6424 mL 3.2120 mL 6.4241 mL 16.0601 mL
    10 mM 0.3212 mL 1.6060 mL 3.2120 mL 8.0301 mL
    15 mM 0.2141 mL 1.0707 mL 2.1414 mL 5.3534 mL
    20 mM 0.1606 mL 0.8030 mL 1.6060 mL 4.0150 mL
    25 mM 0.1285 mL 0.6424 mL 1.2848 mL 3.2120 mL
    30 mM 0.1071 mL 0.5353 mL 1.0707 mL 2.6767 mL
    40 mM 0.0803 mL 0.4015 mL 0.8030 mL 2.0075 mL
    50 mM 0.0642 mL 0.3212 mL 0.6424 mL 1.6060 mL
    60 mM 0.0535 mL 0.2677 mL 0.5353 mL 1.3383 mL
    80 mM 0.0402 mL 0.2008 mL 0.4015 mL 1.0038 mL
    100 mM 0.0321 mL 0.1606 mL 0.3212 mL 0.8030 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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    Product Name:
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