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

SR-3029 

Cat. No.: HY-100011 Purity: 99.58%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 203 In-stock
Estimated Time of Arrival: December 31
2 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 192 In-stock
Estimated Time of Arrival: December 31
10 mg USD 312 In-stock
Estimated Time of Arrival: December 31
25 mg USD 660 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1056 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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 MCE. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531. 

    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 MCE. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531. 

    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 MCE. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531. 

    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.

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

    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.

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    • Biological Activity

    • Protocol

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    • 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)

    CKIϵ

    260 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].

    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].

    Molecular Weight

    480.45

    Formula

    C₂₃H₁₉F₃N₈O

    CAS No.

    1454585-06-8

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (62.44 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" 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
    10 mM 0.2081 mL 1.0407 mL 2.0814 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.58%

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    SR-3029
    Cat. No.:
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