Pyridone 6
Based on 12 publication(s) in Google Scholar
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.
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- 純度: 98.20%
- CAS 番号: 457081-03-7
- 分子式: C18H16FN3O
- 分子量:309.34
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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溶剤 & 溶解度
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MedChemExpress（MCE）の使用を引用している文献 Pyridone 6
More- Sci Immunol. 2024 Jul 12;9(97):eadn0178. [Abstract]
- Sci Adv. 2024 Mar 22;10(12):eadl0368. [Abstract]
- Cell Death Dis. 2025 Aug 7;16(1):595. [Abstract]
- Leukemia. 2012 Oct;26(10):2233-44. [Abstract]
- Mol Syst Biol. 2022 Aug;18(8):e10855. [Abstract]
- Cell Regen. 2021 Mar 3;10(1):8. [Abstract]
- Viruses. 2021 May 25;13(6):976. [Abstract]
- bioRxiv. 2026 Apr 1:2026.03.31.715684. [Abstract]
- bioRxiv. July 29, 2021.
- Patent. US20160368910A1.
- Patent. US20140309249A1.
- Chem Biol. 2012 Jan 27;19(1):140-54. [Abstract]
Customer Validation & Images
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WB
生物活性
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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) |
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
>10 μM
Compound: S30
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Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method
Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method
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[PMID: 26088337] |
| CAL-33 | IC50 |
1.3 μM
Compound: 6
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Growth inhibition of human CAL33 cells
Growth inhibition of human CAL33 cells
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[PMID: 25288188] |
| CTLL | IC50 |
3.1 μM
Compound: 6
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Inhibition of PMA-induced murine T cell lymphoma cell proliferation
Inhibition of PMA-induced murine T cell lymphoma cell proliferation
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[PMID: 11934592] |
| FaDu | IC50 |
2.4 μM
Compound: 6
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Growth inhibition of human FADU cells
Growth inhibition of human FADU cells
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[PMID: 25288188] |
| U-266 | IC50 |
250 nM
Compound: 16
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Antiproliferative activity against human U266B1 cells assessed as inhibition of cell proliferation
Antiproliferative activity against human U266B1 cells assessed as inhibition of cell proliferation
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[PMID: 32120325] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 457081-03-7
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性状 Solid
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分子量 309.34
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分子式 C18H16FN3O
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Color Light brown to brown
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SMILES
FC1=CC2=C(C(NC=C3)=O)C3=C(N=C(C(C)(C)C)N4)C4=C2C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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Sci Immunol
2024 Jul 12;9(97):eadn0178. PMID: 38996010 -
Sci Adv
2024 Mar 22;10(12):eadl0368. PMID: 38507500 -
Cell Death Dis
Activation of AKT via a dual mechanism enhances the susceptibility of melanoma cells to glucose deprivation. [Abstract]2025 Aug 7;16(1):595. PMID: 40774947 -
Leukemia
Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib/multi-targeted inhibitors and JAK inhibitors. [Abstract]2012 Oct;26(10):2233-44. PMID: 22469781
Pyridone 6 purchased from MedChemExpress. Usage Cited in: Leukemia. 2012 Oct;26(10):2233-44. [Abstract]
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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Mol Syst Biol
Drug-microenvironment perturbations reveal resistance mechanisms and prognostic subgroups in CLL. [Abstract]2022 Aug;18(8):e10855. PMID: 35959629 -
Cell Regen
RhoA/Rock activation represents a new mechanism for inactivating Wnt/β-catenin signaling in the aging-associated bone loss. [Abstract]2021 Mar 3;10(1):8. PMID: 33655459 -
Viruses
Activation of the STAT3 Signaling Pathway by the RNA-Dependent RNA Polymerase Protein of Arenavirus. [Abstract]2021 May 25;13(6):976. PMID: 34070281 -
bioRxiv
Efficient Generation of Functional TCRαβ+ Cytotoxic T Cells from hiPSCs via Small-Molecule Modulation. [Abstract]2026 Apr 1:2026.03.31.715684. PMID: 41959015 -
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Chem Biol
2012 Jan 27;19(1):140-54. PMID: 22284361
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (323.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
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参考文献
[1]. Thompson JE, et al. Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. Bioorg Med Chem Lett. 2002 Apr 22;12(8):1219-23. [Content Brief]
[2]. Nakagawa R, et al. Pyridone 6, a pan-JAK inhibitor, ameliorates allergic skin inflammation of NC/Nga mice via suppression of Th2 and enhancement of Th17. J Immunol. 2011 Nov 1;187(9):4611-20. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2327 mL | 16.1634 mL | 32.3269 mL | 80.8172 mL |
| 5 mM | 0.6465 mL | 3.2327 mL | 6.4654 mL | 16.1634 mL | |
| 10 mM | 0.3233 mL | 1.6163 mL | 3.2327 mL | 8.0817 mL | |
| 15 mM | 0.2155 mL | 1.0776 mL | 2.1551 mL | 5.3878 mL | |
| 20 mM | 0.1616 mL | 0.8082 mL | 1.6163 mL | 4.0409 mL | |
| 25 mM | 0.1293 mL | 0.6465 mL | 1.2931 mL | 3.2327 mL | |
| 30 mM | 0.1078 mL | 0.5388 mL | 1.0776 mL | 2.6939 mL | |
| 40 mM | 0.0808 mL | 0.4041 mL | 0.8082 mL | 2.0204 mL | |
| 50 mM | 0.0647 mL | 0.3233 mL | 0.6465 mL | 1.6163 mL | |
| 60 mM | 0.0539 mL | 0.2694 mL | 0.5388 mL | 1.3470 mL | |
| 80 mM | 0.0404 mL | 0.2020 mL | 0.4041 mL | 1.0102 mL | |
| 100 mM | 0.0323 mL | 0.1616 mL | 0.3233 mL | 0.8082 mL |
Pyridone 6 関連分類
HY-14435 関連分類
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