Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
SKU | Size | Availability | Price | Qty |
---|---|---|---|---|
G655324-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $165.90 |
Specifications & Purity | 10mM in DMSO |
---|---|
Storage Temp | Store at -80°C |
Shipped In | Ice chest + Ice pads |
Product 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 MRSA:methicillin-resistant S. aureus ; MSSA: methicillin-sensitive S. aureus 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. GW779439X has growth inhibition effects on the AGP-01 cell line (IC 50 = 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. IC50& Target:Aurora A|Stk1|apoptosis |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Canonical SMILES | CN1CCN(CC1)C2=C(C=C(C=C2)NC3=NC=CC(=N3)C4=C5C=CC=NN5N=C4)C(F)(F)F |
---|---|
Molecular Weight | 454.46 |
Enter Lot Number to search for COA: