1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. Pyridone 6

Pyridone 6 

Cat. No.: HY-14435 Purity: 98.04%
Handling Instructions

Pyridone 6 is a pan-JAK inhibitor, which potently inhibits the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, 5 nM for JAK3, and 15 nM for JAK1, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.

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

Pyridone 6 Chemical Structure

Pyridone 6 Chemical Structure

CAS No. : 457081-03-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 245 In-stock
Estimated Time of Arrival: December 31
2 mg USD 144 In-stock
Estimated Time of Arrival: December 31
5 mg USD 235 In-stock
Estimated Time of Arrival: December 31
10 mg USD 324 In-stock
Estimated Time of Arrival: December 31
50 mg USD 946 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Pyridone 6 purchased from MCE. Usage Cited in: Leukemia. 2012 Oct;26(10):2233-44.

    SCM stimulation of phospho-STAT5 and drug combination effect on phosphorylation of phospho-STAT5. Expression of phospho-STAT5 and total STAT5 in MOLM13 cells treated for 1.5 h with DMSO vehicle, PKC412 (5 nM), KIN40 (82.5 nM) or a combination of both. Results shown are representative of two independent experiments in which similar results are observed.

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    Description

    Pyridone 6 is a pan-JAK inhibitor, which potently inhibits the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, 5 nM for JAK3, and 15 nM for JAK1, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.

    IC50 & Target[1][2]

    JAK2

    1 nM (IC50)

    Tyk2

    1 nM (IC50)

    JAK3

    5 nM (IC50)

    Murine JAK1

    15 nM (IC50)

    CDK2

    3.3 μM (IC50)

    cAMP-dependent kinase

    7.1 μM (IC50)

    Csk

    2.1 μM (IC50)

    Hck

    7.7 μM (IC50)

    Fyn T

    0.5 μM (IC50)

    p38

    11 μM (IC50)

    MAPK

    1.78 μM (IC50)

    Mek

    0.16 μM (IC50)

    IκB Kinase 2

    0.3 μM (IC50)

    KDR

    1.4 μM (IC50)

    Flt-1

    1.52 μM (IC50)

    Flt-4

    0.69 μM (IC50)

    FGFR

    1.48 μM (IC50)

    FGFR2

    0.94 μM (IC50)

    Tek

    24 μM (IC50)

    PDGFR

    1.49 μM (IC50)

    PKC(α)

    1.2 μM (IC50)

    In Vitro

    Pyridone 6 is tested as an inhibitor of 21 other protein kinases; Pyridone 6 inhibits these kinases with IC50s ranging from 130 nM to >10 μM. Pyridone 6 inhibits IL2 driven proliferation of CTLL cells with IC50=0.1 μM and IL4 driven proliferation with IC50=0.052 μM[1]. Pyridone 6 (P6) is shown to inhibit kinase by interacting within the ATP-binding cleft of each JAK. The IC50 of Pyridone 6 is 3 nM for all of these cytokines; this is comparable to the reported IC50s of Pyridone 6 for JAK2, Tyk2, and JAK3. Pyridone 6 strongly inhibits Th2 and modestly inhibits Th1, whereas it enhances Th17 development when present within a certain range of concentrations. Pyridone 6 reduces IFN-γ and IL-13, whereas it enhances IL-17 and IL-22 expression. Pyridone 6 also inhibits both Th1 and Th2 development, whereas it promotes Th17 differentiation from naive T cells when present within a certain range of concentrations[2].

    In Vivo

    Pyridone 6 (P6) delays the onset and reduced the magnitude of skin disease in an AD-like skin-disease model of NC/Nga mice. P6-nano strongly ameliorates atopic dermatitis (AD) in NC/Nga mice, exerting an effect comparable to that of betamethasone ointment, a commonly used drug, which also tested as a positive control. In contrast, empty polylactic acid with glycolic acid (PLGA) nanoparticles (C-nano) seemed to have no effect[2].

    Molecular Weight

    309.34

    Formula

    C₁₈H₁₆FN₃O

    CAS No.

    457081-03-7

    SMILES

    FC1=CC2=C(C(NC=C3)=O)C3=C(N=C(C(C)(C)C)N4)C4=C2C=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 : ≥ 100 mg/mL (323.27 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 3.2327 mL 16.1634 mL 32.3269 mL
    5 mM 0.6465 mL 3.2327 mL 6.4654 mL
    10 mM 0.3233 mL 1.6163 mL 3.2327 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 (8.08 mM); Clear solution

    • 2.

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

      Solubility: 2.5 mg/mL (8.08 mM); Suspended solution; Need ultrasonic

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (8.08 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [2]

    Naive CD4+ T cells are treated with various concentrations of Pyridone 6 (10 and 30 nM) in RPMI 1640 medium 1 h before the appropriate cytokines are added to create each Th-differentiating condition. Immunoblotting is performed using antiphospho-STAT protein Abs or anti-total STAT protein Abs[2].

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

    Animal Administration
    [2]

    Mice[2]
    NC/Nga mice are used at the age of 10-15 wk. To assess the effect of Pyridone 6 treatment on AD symptoms, nanoparticles containing Pyridone 6 (2 mg/body) or empty nanoparticles as a negative control (C-nano) are dissolved in 0.1 mL saline and administered s.c. 1 d after Dfb ointment application; this treatment is repeated twice a week. To assess the effects of recombinant murine IL-17 and IL-22, these cytokines (50 μg/kg) or 100 μL PBS is administered for the same duration as the nanoparticles. Twenty milligrams of 0.064% betamethasone ointment are applied to the dorsal lesion of mice once a week[2].

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

    References
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    Keywords:

    Pyridone 6Pyridone6Pyridone-6JAKJanus kinaseInhibitorinhibitorinhibit

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    Product name:
    Pyridone 6
    Cat. No.:
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