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

GW779439X 

Cat. No.: HY-103645
Handling Instructions

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

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10 mM * 1 mL in DMSO Check price and availability
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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

 

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.

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

Molecular Weight

454.45

Formula

C₂₂H₂₁F₃N₈

CAS No.
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)

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
10 mM 0.2200 mL 1.1002 mL 2.2005 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are provided by MCE.
References
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Keywords:

GW779439XBacterialAurora KinaseApoptosispazolopyridazinederivatives serinethreoninekinaseStk1βlactamresistantcancerInhibitorinhibitorinhibit

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