2. Anti-infection Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. Bacterial Aurora Kinase Apoptosis
  4. GW779439X

GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway. MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus

For research use only. We do not sell to patients.

GW779439X Chemical Structure

GW779439X Chemical Structure

CAS No. : 551919-98-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 In-stock
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 250 In-stock
25 mg USD 550 In-stock
50 mg USD 900 In-stock
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Based on 1 publication(s) in Google Scholar

GW779439X Related Antibodies

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Aurora Kinase Aurora A Aurora B Aurora C

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway[1][2]. MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus

IC50 & Target[1][2]

Aurora A

 

Stk1

 

apoptosis

 

Cellular Effect
Cell Line Type Value Description References
THP-1 CC50
< 0.05 μM
Compound: 1, GW779439X
Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
[PMID: 35035774]
In Vitro

GW779439X (2 μM) biochemically inhibits Stk1. GW779439X (5 μM) potentiates ceftaroline activity against a ceftaroline-resistant MRSA strain. GW779439X is able to potentiate the activity of oxacillin against various S. aureus isolates, including both MRSA and MSSA isolates, but the potentiation is clearly strongest in PBP2A-containing strains[1].
GW779439X has growth inhibition effects on the AGP-01 cell line (IC50= 0.57 μM). GW779439X (1μM) significantly blockS the cell cycle at the G0/G1 phase and sub-G1 phase. GW779439X (1μM; 72 hours; AGP-01 cells) significantly decreases expression levels of genes involved in proliferation progression (c-MYC, NRAS, and CDC25A) and increases expression levels of genes involved in cell cycle blocking (CDKN1A and TP53)[2.

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

GW779439X Related Antibodies
Molecular Weight

454.45

Formula

C22H21F3N8
CAS No.
Appearance

Solid

Color

White to light brown

SMILES

FC(C1=CC(NC2=NC=CC(C3=C4C=CC=NN4N=C3)=N2)=CC=C1N5CCN(C)CC5)(F)F
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
In Vitro: 

DMSO : 31.25 mg/mL (68.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2005 mL 11.0023 mL 22.0046 mL
5 mM 0.4401 mL 2.2005 mL 4.4009 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.85%

SDS (251 KB)

COA (254 KB) HNMR (285 KB) LCMS (91 KB)

Handling Instructions (2659 KB)
References

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 2.2005 mL 11.0023 mL 22.0046 mL 55.0116 mL
5 mM 0.4401 mL 2.2005 mL 4.4009 mL 11.0023 mL
10 mM 0.2200 mL 1.1002 mL 2.2005 mL 5.5012 mL
15 mM 0.1467 mL 0.7335 mL 1.4670 mL 3.6674 mL
20 mM 0.1100 mL 0.5501 mL 1.1002 mL 2.7506 mL
25 mM 0.0880 mL 0.4401 mL 0.8802 mL 2.2005 mL
30 mM 0.0733 mL 0.3667 mL 0.7335 mL 1.8337 mL
40 mM 0.0550 mL 0.2751 mL 0.5501 mL 1.3753 mL
50 mM 0.0440 mL 0.2200 mL 0.4401 mL 1.1002 mL
60 mM 0.0367 mL 0.1834 mL 0.3667 mL 0.9169 mL
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GW779439X Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GW779439X551919-98-3BacterialAurora KinaseApoptosispazolopyridazinederivatives serinethreoninekinaseStk1βlactamresistantcancerInhibitorinhibitorinhibit

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