1. Cell Cycle/DNA Damage Stem Cell/Wnt
  2. Casein Kinase
  3. SR-3029

SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively, and Kis of 97 nM for both kinases.

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

SR-3029 Chemical Structure

SR-3029 Chemical Structure

CAS No. : 1454585-06-8

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 127 In-stock
Solution
10 mM * 1 mL in DMSO USD 127 In-stock
Solid
2 mg USD 70 In-stock
5 mg USD 120 In-stock
10 mg USD 190 In-stock
25 mg USD 380 In-stock
50 mg USD 610 In-stock
100 mg USD 980 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    SR-3029 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531.   [Abstract]

    SR3029 suppresses TPA-induced skin tumor formation in vivo via blockade of Wnt/β-catenin signaling in mouse skin two-stage chemical carcinogenesis. Fifteen mice per group are initiated with DMBA, followed by repetitive applications of TPA alone or together with SR3029 in acetone twice a week for 18 wk. Hematoxylin/eosin staining and immunohistochemistry staining using antibodies specific for Ki-67, β-catenin, active β-catenin, CK1ε, and CK1δ.

    SR-3029 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531.   [Abstract]

    SR3029 suppresses TPA-induced skin tumor formation in vivo via blockade of Wnt/β-catenin signaling in mouse skin two-stage chemical carcinogenesis. Fifteen mice per group are initiated with DMBA, followed by repetitive applications of TPA alone or together with SR3029 in acetone twice a week for 18 wk. The mRNA expression levels of CD44, cyclin D1, and Fosb in tumor tissuesare quantitated by real-time PCR.

    SR-3029 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531.   [Abstract]

    SR3029 suppresses TPA-induced skin tumor formation in vivo via blockade of Wnt/β-catenin signaling in mouse skin two-stage chemical carcinogenesis. Fifteen mice per group are initiated with DMBA, followed by repetitive applications of TPA alone or together with SR3029 in acetone twice a week for 18 wk. Expression levels of β-catenin, active β-catenin, CK1ε, CK1δ, and LRP6 in tumor samples are visualized after immunoblotting.

    SR-3029 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531.   [Abstract]

    TPA induces the phosphorylation of LRP6 and the formation of a CK1ε-LRP6-axin1 complex. (A) HEK293T and UACC903 cells cotransfected with CK1ε-GFP and LRP6 expression vectors are treated with 10 nM TPA for 6 h. Cell lysates are analyzed by immunoblotting. (B) HEK293T and UACC903 cells transfected with a CK1εexpression plasmid ae treated with or without 10 nM TPA for 6 h. (C) UACC903 cells are incubated with 10 nM TPA in the presence or absence of 60 nM SR3029 for 6 h.

    SR-3029 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531.   [Abstract]

    TPA increases the expression of Wnt target genes. HEK293T and UACC903 cells are treated for 24 h with or without 10 nM TPA in the presence or absence of increasing concentrations of SR3029 as indicated. Quantitative PCR analysis is conducted to detect the mRNA expression of CD44, cyclin D1, and DKK1.

    View All Casein Kinase Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively, and Kis of 97 nM for both kinases.

    IC50 & Target[1]

    CKIδ

    44 nM (IC50)

    CDK6/cyclin D3

    427 nM (IC50)

    CDK6/cyclin D1

    428 nM (IC50)

    CDK4/cyclin D3

    368 nM (IC50)

    CDK4/cyclin D1

    576 nM (IC50)

    FLT3

    3000 nM (IC50)

    In Vitro

    SR-3029 is a potent CK1δ/CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively. SR-3029 is ATP competitive, with Kis of 97 nM for CK1δ/CK1ε. SR-3029 also blocks CDK6/cyclin D3, CDK6/cyclin D1, CDK4/cyclin D3, CDK4/cyclin D1 and FLT3, with IC50s of 427, 428, 368, 576, and 3000 nM, respectively. SR-3029 shows inhibitory effects on A375 cells, with an EC50 of 86 nM[1]. CK1δ is a necessary and sufficient driver of Wnt/β-catenin signaling in human breast cancer. SR-3029 shows less potent activities against MCF7 and T47D breast cancer cells and the MCF10A cell line, which express low amounts of CK1δ[2].

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

    In Vivo

    SR-3029 (20 mg/kg daily i.p.) exibits anti-tumor effects in rthotopic MDA-MB-231, MDA-MB-468 (TNBC), SKBR3 and BT474 (HER2+) tumor xenografts with no overt toxicity in mice. SR-3029 (20 mg/kg daily i.p.) also effectively inhibits the growth of tumor in primary patient-derived xenograft (PDX) models. In addition, SR-3029 (20 mg/kg, i.p.) strongly reduces the expression of nuclear β-catenin in tumors of mice[2].

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

    Molecular Weight

    480.45

    Formula

    C23H19F3N8O

    CAS No.
    Appearance

    Solid

    Color

    White to pink

    SMILES

    FC1=CC(N2C=NC3=C(NCC4=NC5=CC=C(F)C(F)=C5N4)N=C(N6CCOCC6)N=C23)=CC=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 : ≥ 30 mg/mL (62.44 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 2.0814 mL 10.4069 mL 20.8138 mL
    5 mM 0.4163 mL 2.0814 mL 4.1628 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
    ×
    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:

    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: ≥ 2.08 mg/mL (4.33 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

      Solubility: ≥ 2.08 mg/mL (4.33 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    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).
    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: 99.41%

    References
    Kinase Assay
    [1]

    Briefly, final assay concentrations for CK1δ, Ulight peptide substrate (ULight-Topo-Ila(Thr1342) peptide) and ATP are 2 nM, 200 nM and 20 μM respectively. The reaction is performed at room temperature in a 10 μL final volume (384-well low volume plate) containing the following: 50 mM Hepes, pH 7.5, 5 mM MgCl2, 0.1 mg/mL bovine serum albumin, 1 mM dl-dithiothreitol, 0.01% Triton X-100 and 1% DMSO. After 10 min, the reaction is terminated by addition of 10 μL of 4 nM Eu-anti-p-Topo-Ila in Lance Detection Buffer. The fluorescent signal is detected using a plate reader. 10 point does-response curves with 3-fold dilutions starting from 10 μM for each compound (SR-3029) is generated in duplicate and data fit to a four parameter logistic[1].

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

    Cell Assay
    [1]

    Human A375 melanoma cells are cultured in Dulbecco's Modified Eagle Medium (DMEM) supplemented with 10% fetal bovine serum, 1% penicillin/streptomycin and 1× MEM Non-Essential Amino Acids at 37°C, 5% CO2. To evaluate the anti-proliferative activity of newly synthesized CK1δ/ε inhibitors, each compound (SR-3029) is subjected to MTT assays against A375 melanoma cells and their EC50 values are determined. Briefly, A375 melanoma cells are plated into a 96-well plate and treated with a series of concentrations of each new inhibitor, vehicle (DMSO) or with SR-3029 or SR-1277 (positive controls). MTT assays are performed four days after treatment and data are analyzed using the GraphPad Prism5[1].

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

    Animal Administration
    [2]

    Stable pools of MDA-MB-231-Luc, MDA-MB-231, MDA-MB-468, SKBR3, or BT474 cells are established by injection of 2 × 106 cancer cells into the mammary fat pads of 6-week-old female athymic nude mice. Establishment of BCM-4013 patient-derived xenografts is performed. Briefly, fresh xenograft tumor fragments (∼1 mm3) are transplanted into the cleared mammary fat pad of recipient SCID/Bg mice. Mice are treated with SR-3029 or vehicle (10:10:80, DMSO:Tween-80:Water) at 20 mg/kg daily by i.p. injection. Tumor volumes are measured as the indicated intervals using calipers or by luminescence imaging with the IVIS 100 imager after subcutaneous injection of luciferin (15 mg/mL). Average radiance (p/s/cm2/sr) is determined from tumor region-of-interest (ROI) using Living-Image analysis software[2].

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

    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 2.0814 mL 10.4069 mL 20.8138 mL 52.0345 mL
    5 mM 0.4163 mL 2.0814 mL 4.1628 mL 10.4069 mL
    10 mM 0.2081 mL 1.0407 mL 2.0814 mL 5.2035 mL
    15 mM 0.1388 mL 0.6938 mL 1.3876 mL 3.4690 mL
    20 mM 0.1041 mL 0.5203 mL 1.0407 mL 2.6017 mL
    25 mM 0.0833 mL 0.4163 mL 0.8326 mL 2.0814 mL
    30 mM 0.0694 mL 0.3469 mL 0.6938 mL 1.7345 mL
    40 mM 0.0520 mL 0.2602 mL 0.5203 mL 1.3009 mL
    50 mM 0.0416 mL 0.2081 mL 0.4163 mL 1.0407 mL
    60 mM 0.0347 mL 0.1734 mL 0.3469 mL 0.8672 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    SR-3029 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.

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email Address *

    Phone Number *

     

    Organization Name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    SR-3029
    Cat. No.:
    HY-100011
    Quantity:
    MCE Japan Authorized Agent: