1. Protein Tyrosine Kinase/RTK
  2. Syk
  3. R406

R406 

Cat. No.: HY-12067 Purity: 96.88%
Handling Instructions

R406 is a competitive Syk inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value.

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

R406 Chemical Structure

R406 Chemical Structure

CAS No. : 841290-81-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 166 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 720 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of R406:

Top Publications Citing Use of Products

    R406 purchased from MCE. Usage Cited in: J Pharmacol Sci. 2017 May;134(1):29-36.

    The effects of R406 treatment on the phosphorylation of 3BP2 and p38MAPK in white blood cells from the spleens of NZB/W F1 mice. (A) The phosphorylation of the 3BP2 and (B) the phosphorylation of p38MAPK in the renal cortex of control and R406-treated mice.

    R406 purchased from MCE. Usage Cited in: Cell. 2018 Oct 4;175(2):442-457.e23.

    Syk inhibitors (R406 and Piceatannol) are added during the induction of trastuzumab-dependent BT-474 phagocytosis. The binding of the phagosome marker Rab7 to AIM2 in macrophages are evaluated by co-immunoprecipitation.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    R406 is a competitive Syk inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value.

    IC50 & Target

    Ki: 30 nM (Syk)[1]
    IC50: 41 nM (Syk)[1]

    In Vitro

    R406 also exhibits antagonistic activity for adenosine A3 receptor with an IC50 estimated to be 93 nM[1]. In Ramos B lymphoma cells, B-cell receptor (BCR) crosslinking induces robust phosphorylation of B-cell linker protein (BLNK), which is ablated by addition of the Syk inhibitor R406. Additionally, R406 significantly reduces constitutive Syk signaling in EBV+ cell lines derived from patients with Post-transplant lymphoproliferative disorder (PTLD), termed SLCL. Therefore, R406 inhibits Syk activation[2].

    In Vivo

    Prophylactic treatment of mice with R406 administers 1 h before immune complex challenge reduces the cutaneous reverse passive Arthus reaction by approximately 72 and 86% at 1 and 5 mg/kg, respectively, compared with the vehicle control. The net optical density reading of extravasated dye extracted after treatment with R406 at 1 or 5 mg/kg R406 is reduced from 0.14 (vehicle) to 0.04 or 0.02, respectively (p<0.01)[1].

    Molecular Weight

    628.63

    Formula

    C₂₈H₂₉FN₆O₈S

    CAS No.

    841290-81-1

    SMILES

    COC1=CC(NC2=NC(NC3=NC(N4)=C(C=C3)OC(C)(C)C4=O)=C(C=N2)F)=CC(OC)=C1OC.OS(C5=CC=CC=C5)(=O)=O

    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 : ≥ 61 mg/mL (97.04 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 1.5908 mL 7.9538 mL 15.9076 mL
    5 mM 0.3182 mL 1.5908 mL 3.1815 mL
    10 mM 0.1591 mL 0.7954 mL 1.5908 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: ≥ 2.5 mg/mL (3.98 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (3.98 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [1]

    The fluorescence polarization reactions are performed. For Kidetermination, duplicate 200 μL reactions are set up at eight different ATP concentrations from 200 μM (2-fold serial dilutions) in the presence of either DMSO or R406 at 125, 62.5, 31.25, 15.5, or 7.8 nM. At different time points, 20 μL of each reaction is removed and quenched to stop the reaction. For each concentration of R406, the rate of reaction at each concentration of ATP is determined and plotted against the ATP concentration to determine the apparent Km and Vmax (maximal rate). Finally the apparent Km (or apparent Km/Vmax) is plotted against the inhibitor concentration to determine the Ki. All data analysis is performed using Prism and Prism enzyme kinetics programs[1]

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

    Cell Assay
    [2]

    Cells (0.5-1×106 cells/mL) are plated in serial dilutions of small molecule inhibitors R406, LY294002, or PD98059 (0-10 μM), or equivalent amounts of vehicle (DMSO, 0-1:1000). Drug and media are replenished after 48 h of a total of 96 h in culture at 37°C. Cell cycle analysis using propidium iodide. The percentage of apoptotic cells is determined using Annexin V-enhanced GFP (EGFP) apoptosis detection kits. Data is analyzed on a FACScan flow cytometer[2].

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

    Animal Administration
    [1]

    Mice[1]
    Mice are challenged intravenously with 1% ovalbumin (OVA) in saline (10 mg/kg) containing 1% Evans blue dye. Ten minutes later, mice are anesthetized with isofluorane and shaved dorsolaterally. The rabbit anti-OVA IgG (50 μg/25 μL) is injected intradermally on the left side of the back at three adjacent locations. Three injections of rabbit polyclonal IgG (50 μg/25 μL) on the opposite side of the same animal served as controls. R406 (1 and 5 mg/kg) or vehicle (67% PEG 400) is administered to animals 60 min before antibody/antigen challenge. Four hours after challenge, the animals are euthanized, and skin tissue is assessed for edema and inflammation by measuring dye extravasation into the surrounding tissue. Punch biopsy of the injection sites (8 mm) are incubated in 2 mL of formamide at 80°C overnight. The concentration of the extravasated Evans blue dye is measured spectrophotometrically at OD610.

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

    References
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    Product Name:
    R406
    Cat. No.:
    HY-12067
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