Art. -Nr.: HY-13450

ZM 449829

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ZM 449829 is a potent, selective and ATP competitive inhibitor of JAK3, with a pIC₅₀ of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of the JAK3.

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Reinheit: 99.73%
CAS. Nr.: 4452-06-6
Formel: C₁₃H₁₀O
Molecular Weight:182.22

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ZM 449829 Chemical Structure

CAS. Nr.: 4452-06-6

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

Biologische Aktivität

Beschreibung

ZM 449829 is a potent, selective and ATP competitive inhibitor of JAK3, with a pIC₅₀ of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of the JAK3^[1].

IC₅₀ & Target^[1]

JAK3

6.8 (pIC₅₀)

JAK1

4.7 (pIC₅₀)

EGFR

5.0 (pIC₅₀)

Alle JAK Isoform-spezifische Produkte anzeigen :

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL10-induced Stat3 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL10-induced Stat3 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL10-induced Stat3 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL10-induced Stat3 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL15-induced Stat5 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL15-induced Stat5 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL15-induced Stat5 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL15-induced Stat5 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL4-induced Stat5 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL4-induced Stat5 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL4-induced Stat5 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL4-induced Stat5 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL4-induced Stat6 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL4-induced Stat6 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL4-induced Stat6 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL4-induced Stat6 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL6-induced Stat1 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL6-induced Stat1 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL6-induced Stat1 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL6-induced Stat1 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL6-induced Stat3 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL6-induced Stat3 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL6-induced Stat3 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL6-induced Stat3 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL7-induced Stat5 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL7-induced Stat5 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated IL7-induced Stat5 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated IL7-induced Stat5 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated interferon-gamma-induced Stat1 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated interferon-gamma-induced Stat1 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry	[PMID: 18157122]
T-cell	IC₅₀	<20 μM Compound: 12, ZM, ZM-449829	Inhibition of JAK-mediated interferon-gamma-induced Stat1 phosphorylation in BALB/c mouse CD8++ T cells by Phospho-Flow cytometry Inhibition of JAK-mediated interferon-gamma-induced Stat1 phosphorylation in BALB/c mouse CD8++ T cells by Phospho-Flow cytometry	[PMID: 18157122]

In Vitro

ZM 449829 (compound 22) is a very weak inhibitors of EGF-R (pIC₅₀=5.0) , Jak1 (pIC₅₀=4.7), and tyrosine kinases Lck and CDK4 (pIC₅₀ <5.0)^[1].
ZM449829 (1 μM; 30 minutes) blocks IL-2-induced STAT5 phosphorylation^[2].

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

Western Blot Analysis^[2]

Cell Line:

YTS, NK92, and ex vivo NK cells
Concentration:

1 μM
Incubation Time:

30 minutes pretreatment
Result:

Inhibits the phosphorylation of STAT5.

Chemical Information

CAS. Nr. 4452-06-6
Appearance Solid
Molecular Weight 182.22
Formel C₁₃H₁₀O
Color White to off-white
SMILES

C=CC(C1=CC=C2C=CC=CC2=C1)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (548.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

5.4879 mL

27.4394 mL

54.8787 mL

5 mM

1.0976 mL

5.4879 mL

10.9757 mL

10 mM

0.5488 mL

2.7439 mL

5.4879 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (13.72 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (13.72 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 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]. Brown GR, et, al. Naphthyl ketones: a new class of Janus kinase 3 inhibitors. Bioorg Med Chem Lett. 2000 Mar 2010(6)575-9. [Content Brief]

[2]. Orange JS, et, al. IL-2 induces a WAVE2-dependent pathway for actin reorganization that enables WASp-independent human NK cell function. J Clin Invest. 2011 Apr; 121(4): 1535-48. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	5.4879 mL	27.4394 mL	54.8787 mL	137.1968 mL
	5 mM	1.0976 mL	5.4879 mL	10.9757 mL	27.4394 mL
	10 mM	0.5488 mL	2.7439 mL	5.4879 mL	13.7197 mL
	15 mM	0.3659 mL	1.8293 mL	3.6586 mL	9.1465 mL
	20 mM	0.2744 mL	1.3720 mL	2.7439 mL	6.8598 mL
	25 mM	0.2195 mL	1.0976 mL	2.1951 mL	5.4879 mL
	30 mM	0.1829 mL	0.9146 mL	1.8293 mL	4.5732 mL
	40 mM	0.1372 mL	0.6860 mL	1.3720 mL	3.4299 mL
	50 mM	0.1098 mL	0.5488 mL	1.0976 mL	2.7439 mL
	60 mM	0.0915 mL	0.4573 mL	0.9146 mL	2.2866 mL
	80 mM	0.0686 mL	0.3430 mL	0.6860 mL	1.7150 mL
	100 mM	0.0549 mL	0.2744 mL	0.5488 mL	1.3720 mL

Keywords

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ZM 449829

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-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-Hepatitis C Virus 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

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Alle JAK Isoform-spezifische Produkte anzeigen

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ZM 449829 Related Classifications

HY-13450 Related Classifications