Art. -Nr.: HY-14435

Pyridone 6

12 Cited Publications

Kundenbewertung

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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Reinheit: 98.20%
CAS. Nr.: 457081-03-7
Formel: C₁₈H₁₆FN₃O
Molecular Weight:309.34

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Pyridone 6 Chemical Structure

CAS. Nr.: 457081-03-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle JAK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>10 μM Compound: S30	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	[PMID: 26088337]
CAL-33	IC₅₀	1.3 μM Compound: 6	Growth inhibition of human CAL33 cells Growth inhibition of human CAL33 cells	[PMID: 25288188]
CTLL	IC₅₀	3.1 μM Compound: 6	Inhibition of PMA-induced murine T cell lymphoma cell proliferation Inhibition of PMA-induced murine T cell lymphoma cell proliferation	[PMID: 11934592]
FaDu	IC₅₀	2.4 μM Compound: 6	Growth inhibition of human FADU cells Growth inhibition of human FADU cells	[PMID: 25288188]
U-266	IC₅₀	250 nM Compound: 16	Antiproliferative activity against human U266B1 cells assessed as inhibition of cell proliferation Antiproliferative activity against human U266B1 cells assessed as inhibition of cell proliferation	[PMID: 32120325]

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].

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

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].

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

Chemical Information

CAS. Nr. 457081-03-7
Appearance Solid
Molecular Weight 309.34
Formel C₁₈H₁₆FN₃O
Color Light brown to brown
SMILES

FC1=CC2=C(C(NC=C3)=O)C3=C(N=C(C(C)(C)C)N4)C4=C2C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

All WB

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Journal Impact Factor

Sci Immunol

Initiator cell death event induced by SARS-CoV-2 in the human airway epithelium. [Abstract]

2024 Jul 12;9(97):eadn0178. PMID: 38996010
Sci Adv

JAK/STAT signaling pathway affects CCR5 expression in human CD4+ T cells. [Abstract]

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.
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
bioRxiv

July 29, 2021.
Patent

US20160368910A1.
Patent

US20140309249A1.
Chem Biol

Discovery of potent and selective covalent inhibitors of JNK. [Abstract]

2012 Jan 27;19(1):140-54. PMID: 22284361

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 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

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.

Protocol 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

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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].

MedChemExpress (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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Pyridone 6

12 Cited Publications

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Pyridone 6

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Autoimmune Disease Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) Pyridone 6

Alle JAK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pyridone 6 Related Classifications

HY-14435 Related Classifications