ZM 449829
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.73%
- CAS No.: 4452-06-6
- Formula: C13H10O
- Molecular Weight:182.22
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All EGFR Isoforms
More
Biological Activity
|
JAK3 6.8 (pIC50) |
JAK1 4.7 (pIC50) |
EGFR 5.0 (pIC50) |
|
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] |
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.
-
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 No. 4452-06-6
-
Appearance Solid
-
Molecular Weight 182.22
-
Formula C13H10O
-
Color White to off-white
-
SMILES
C=CC(C1=CC=C2C=CC=CC2=C1)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 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.
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:
-
-
-
-
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
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.
Purity & Documentation
-
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)
-
Handling Instructions (2659 KB)
References
[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]
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, 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 |