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Pyridone 6

Pyridone 6
Pyridone 6 (JAK Inhibitor)(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.
Catalog No. T3080Cas No. 457081-03-7
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Purity:98.74%
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Pyridone 6

Catalog No. T3080Cas No. 457081-03-7
Pyridone 6 (JAK Inhibitor)(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.
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Pack SizePriceAvailabilityQuantity
1 mg$75In Stock
2 mg$108In Stock
5 mg$165In Stock
10 mg$233In Stock
25 mg$473In Stock
50 mg$693In Stock
100 mg$988In Stock
500 mg$1,980In Stock
1 mL x 10 mM (in DMSO)$186In Stock
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Product Introduction

Bioactivity
Description
Pyridone 6 (JAK Inhibitor)(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.
Targets&IC50
JAK1:15 nM, JAK2:1 nM, JAK3:5 nM(Ki), TYK2:1 nM
In vitro
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[1]. Pyridone 6 inhibits osteoclast differentiation in mouse bone marrow macrophage (BMM) cultures stimulated by the receptor activator of nuclear factor-k B (NF-k B) ligand (RANKL) and co-cultures of bone marrow cells and osteoblasts. Pyridone 6 suppresses the expression of c-Fos and nuclear factor of activated T cells (NFAT) c1 in BMMs. Pyridone 6 also suppresses I-k B degradation and extracellular signal-regulated kinase (ERK) in mature osteoclasts, suggesting that these are the key molecules that pyridone 6 targets in the inhibition of osteoclast function[2]. Pyridone 6 (P6), is found to inhibit the JAKs in the low nanomolar range (IC50, 1-15 nM) and blocks IL-2-dependent proliferation of CTLL cells. Pyridone 6 is a reversible ATP inhibitor, and when tested against many other kinases, IC50s of >130 nM are required[3].
In vivo
Pyridone 6 (P6) postpones the initiation and diminishes the severity of skin conditions in an AD-like model using NC/Nga mice, effectively mitigating atopic dermatitis (AD) symptoms. Its efficacy is on par with betamethasone ointment, a standard treatment, also serving as a positive control. Conversely, empty PLGA nanoparticles (C-nano) appear ineffective[1].
Kinase Assay
Kinase Assays: Baculovirus-expressed glutathione S-transferase-tagged proteins encoding the intracellular domain of IGF-1R (amino acids 957-1367) and IR (amino acids 979-1382) are used for determinations of IC50s by a homogeneous time-resolved fluorescence assay. A filter binding assay is used for appKi determinations using activated IGF-1R and IR kinases. Expanded kinase-selectivity profiling of GSK1838705A is carried out by screening the compound in the KinaseProfiler panel.
Cell Research
Pyridone 6 (P6) is prepared in DMSO and stored, and then diluted with appropriate medium before use[1]. Naive CD4+ T cells are treated with various concentrations of Pyridone 6 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[1].
AliasJanus-Associated Kinase Inhibitor I, JAK Inhibitor, CMP 6, JAK Inhibitor I
Chemical Properties
Molecular Weight309.34
FormulaC18H16FN3O
Cas No.457081-03-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 12 mg/mL (38.79 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.2327 mL16.1634 mL32.3269 mL161.6344 mL
5 mM0.6465 mL3.2327 mL6.4654 mL32.3269 mL
10 mM0.3233 mL1.6163 mL3.2327 mL16.1634 mL
20 mM0.1616 mL0.8082 mL1.6163 mL8.0817 mL

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