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Pyridone 6

Cat. No. M3737
Pyridone 6 Structure
Synonym:

Merck-5, CMP 6, JAK Inhibitor I

Size Price Availability Quantity
2mg USD 119.7  USD133 In stock
5mg USD 181.8  USD202 In stock
10mg USD 267.3  USD297 In stock
50mg USD 783  USD870 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Pyridone 6 displays potent inhibitory activity against JAK1 (IC50 = 15 nM for murine JAK1), JAK2 (IC50 = 1 nM), JAK3 (Ki = 5 nM), and Tyk2 (IC50 = 1 nM). JAK1 (Janus kinase 1), JAK2 and JAK3 belong to the family of non-receptor janus tyrosine kinases, which regulate a spectrum of cellular functions downstream of activated cytokine receptors in the lympho-hematopoietic system. Immunological stimuli, such as interferons and cytokines, induce recruitment of STAT transcription factors to cytokine receptor-associated JAK1, JAK2 and JAK3. Pyridone 6 inhibited osteoclast differentiation in mouse bone marrow macrophage (BMM) cultures stimulated by the receptor activator of nuclear factor-kappaB (NF-kappaB) ligand (RANKL) and co-cultures of bone marrow cells and osteoblasts. Pyridone 6 suppressed the expression of c-Fos and nuclear factor of activated T cells (NFAT) c1 in BMMs. It also inhibited the bone resorptive activity of mature osteoclasts that was accompanied by disruption of actin rings. Pyridone 6 also suppressed I-kappaB 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 309.34
Formula C18H16FN3O
CAS Number 457081-03-7
Purity >98%
Solubility DMSO 5 mg/mL
Storage at -20°C
References

Pyridone 6, a pan-JAK inhibitor, ameliorates allergic skin inflammation of NC/Nga mice via suppression of Th2 and enhancement of Th17.
Nakagawa R, et al. J Immunol. 2011 Nov 1;187(9):4611-20. PMID: 21957150.

Effects of a Janus kinase inhibitor, pyridone 6, on airway responses in a murine model of asthma.
Matsunaga Y, et al. Biochem Biophys Res Commun. 2011 Jan 7;404(1):261-7. PMID: 21111712.

Structural and thermodynamic characterization of the TYK2 and JAK3 kinase domains in complex with CP-690550 and CMP-6.
Chrencik JE, et al. J Mol Biol. 2010 Jul 16;400(3):413-33. PMID: 20478313.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Pyridone 6, Merck-5, CMP 6, JAK Inhibitor I supplier, JAK, inhibitors

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