Powder: -20°C for 3 years | In solvent: -80°C for 1 year
G-5555 is a potent inhibitor of p21-activated kinase 1 (PAK1) (Kis: 3.7 nM and 11 nM for PAK1 and PAK2, respectively).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 48.00 | |
2 mg | In stock | $ 68.00 | |
5 mg | In stock | $ 89.00 | |
10 mg | In stock | $ 128.00 | |
25 mg | In stock | $ 297.00 | |
50 mg | In stock | $ 528.00 | |
100 mg | In stock | $ 769.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 96.00 |
Description | G-5555 is a potent inhibitor of p21-activated kinase 1 (PAK1) (Kis: 3.7 nM and 11 nM for PAK1 and PAK2, respectively). |
Targets&IC50 | PAK2:11 nM (ki), PAK1:3.7 nM (ki) |
In vitro | G-5555 shows high selectivity for the group I PAKs and it also shows excellent kinase selectivity and inhibits only eight out of the 235 kinases tested other than PAK1 with inhibition >70%: PAK2, PAK3, KHS1, Lck, MST3, MST4, SIK2, and YSK1. The IC50s of G-5555 against SIK2, PAK2, KHS1, MST4, YSK1, MST3, and Lck are 9, 11, 10, 20, 34, 43, 52 nM, respectively. There is a negligible activity for G-5555 against the hERG channel with IC50 more than 10 μM in a patch-clamp assay[1]. G-5555 potently inhibits PAK2 (Ki: 11 nM). G-5555 has obviously greater growth inhibitory activity in cell lines that are PAK-amplified compared to non-amplified lines, in an array of 23 breast cancer cell lines[2]. |
In vivo | G-5555 has low blood clearance and an acceptable half-life. Good oral exposure (AUC = 30 μM?h) and high oral bioavailability (F = 80%) are achieved[1]. G-5555 inhibits phosphorylation of the PAK1/2 downstream substrate mitogen-activated protein kinase 1 (MEK1) S298, in an H292 non-small cell lunger cancer (NSCLC) xenograft study in mice. When administered at an oral dose of 25 mg/kg b.i.d., imparts 60% tumor growth inhibition in this model13 and a PAK1 amplified breast cancer xenograft model, MDAMB-175. [2] |
Molecular Weight | 492.96 |
Formula | C25H25ClN6O3 |
CAS No. | 1648863-90-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 20 mg/mL (40.57 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
bottom
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.
G-5555 1648863-90-4 Cytoskeletal Signaling PAK p21 activated kinases G 5555 Inhibitor G5555 inhibit inhibitor