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GW779439X
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Catalog No. T8866Cas No. 551919-98-3
GW779439X is a pyrazolopyridazine compound that inhibits the S. aureus kinase Stk1 and Aurora kinase A (AURKA). It restores the efficacy of β-lactam antibiotics against methicillin-resistant (MRSA) and methicillin-susceptible (MSSA) S. aureus, often re-sensitizing resistant strains. This antibacterial potentiation is achieved through the induction of apoptosis via caspase-3/7 pathway activation.
GW779439X
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Purity: 97.87%
Catalog No. T8866Cas No. 551919-98-3
GW779439X is a pyrazolopyridazine compound that inhibits the S. aureus kinase Stk1 and Aurora kinase A (AURKA). It restores the efficacy of β-lactam antibiotics against methicillin-resistant (MRSA) and methicillin-susceptible (MSSA) S. aureus, often re-sensitizing resistant strains. This antibacterial potentiation is achieved through the induction of apoptosis via caspase-3/7 pathway activation.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $56 | In Stock | In Stock | |
| 2 mg | $79 | In Stock | In Stock | |
| 5 mg | $122 | In Stock | In Stock | |
| 10 mg | $198 | In Stock | In Stock | |
| 25 mg | $448 | In Stock | In Stock | |
| 50 mg | $658 | - | In Stock | |
| 100 mg | $938 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $133 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:97.87%
Appearance:Solid
Color:Red
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Product Introduction
GW779439X AI Summary
GW779439X exhibits significant and diverse bioactivity across various biological targets and assays. It potently inhibits CDK4 (IC50 = 6.0 nM), CDK2 (IC50 = 4.0 nM), and GSK3-beta (IC50 = 16.0 nM), and shows notable binding affinity for CDK4, GSK-3 beta, mTOR, and Pim1 with Kd values ranging from 4.5 nM to 63.0 nM. Additionally, it demonstrates high inhibition levels against human HepG2 cells, plasmodial strains (Plasmodium falciparum 3D7 and Dd2), and Mycobacterium tuberculosis PknB, with IC50 values ranging up to 1500.0 nM and Ki values, indicating strong immunomodulatory and antimicrobial potential.
GW779439X also exhibits cytotoxic effects on human THP-1 cells (CC50 < 50.0 nM) and zebrafish embryos (0% survival at 5 uM). It possesses moderate lipophilicity with a logD value of 3.71 and demonstrates antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 (EC50 = 15.85 nM). In assays involving thermal stability and protein stabilization, it interacts with CLK proteins, affecting their melting temperatures, which indicates potential modulation of splicing factors.
Moreover, GW779439X has moderate effects in kinase inhibition assays including IKK-alpha, IKK-epsilon, Mer Kinase, PIP5K1, and TBK1, suggesting a broad kinase inhibitory profile. It also affects cell viability differentially across cell lines like HEK293T, human fibroblasts, and U2OS, indicating possibly complex, cell-type-specific growth interactions. Therefore, GW779439X represents a multifaceted bioactive agent with implications in kinase inhibition, antimicrobial activity, and potential therapeutic cytotoxicity, warranting further investigation for its various biological effects and therapeutic opportunities..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | GW779439X is a pyrazolopyridazine compound that inhibits the S. aureus kinase Stk1 and Aurora kinase A (AURKA). It restores the efficacy of β-lactam antibiotics against methicillin-resistant (MRSA) and methicillin-susceptible (MSSA) S. aureus, often re-sensitizing resistant strains. This antibacterial potentiation is achieved through the induction of apoptosis via caspase-3/7 pathway activation. |
| Molecular Weight | 454.45 |
| Formula | C22H21F3N8 |
| Cas No. | 551919-98-3 |
| Smiles | CN1CCN(CC1)c1ccc(Nc2nccc(n2)-c2cnn3ncccc23)cc1C(F)(F)F |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 4.55 mg/mL (10.01 mM), Sonication is recommended.  | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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