- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S7093||IPA-3||<1 mg/mL||70 mg/mL||7 mg/mL|
|S7094||PF-3758309||<1 mg/mL||98 mg/mL||98 mg/mL|
|S8444||KPT-9274||<1 mg/mL||100 mg/mL||100 mg/mL|
|S7271||FRAX597||<1 mg/mL||14 mg/mL||1 mg/mL|
|S7807||FRAX486||<1 mg/mL||22 mg/mL||<1 mg/mL|
|S7989||FRAX1036||<1 mg/mL||<1 mg/mL||20 mg/mL|
- PAK Inhibitors (6)
- New PAK Products
|Catalog No.||Information||Product Use Citations||Product Validations|
IPA-3 is a selective non-ATP competitive Pak1 inhibitor with IC50 of 2.5 μM in a cell-free assay, no inhibition to group II PAKs (PAKs 4-6).
(e) Immunoblot analysis of p-ERM, p-Pak1 and Pak1 in Ishikawa cells treated with various doses of Pak1 inhibitor IPA-3 for 24 h. Actin serves as a loading control
PF-03758309 is a potent, ATP-competitive, pyrrolopyrazole inhibitor of PAK4 with IC50 of 1.3 nM.
Western blot analysis of phosphorylation of ERK, Akt and p38 in lysates from SH-SY5Y and IMR-32 cells treated with serial concentrations of PF-3758309 for 24 h. The phosphorylation of ERK decreased upon PF-3758309 treatment in both cell lines, but no obvious change in the phosphorylation of Akt was observed. The phosphorylation of p38 was increased in the IMR-32 cells treated with PF-3758309, but no obvious change was noted in SH-SY5Y cells.
KPT-9274 is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay.
FRAX597 is a potent, ATP-competitive inhibitor of group I PAKs with IC50 of 8 nM, 13 nM, and 19 nM for PAK1, PAK2, and PAK3, respectively.
(e) FRAX597 (1 μM) for 1 h, and seeded onto Matrigel. 2F-2B cells were supplemented with exosomes (30 μg). After 24 h culture, tube formation was analysed and imaged. Scale bar = 50 μm. (representative images from n=3, *p<0.05, **p<0.01 and NS = no significant difference).
FRAX486 is a potent p21-activated kinase (PAK) inhibitor with IC50 values of 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively.
FRAX-1036 is a potent and selective PAK inhibitor with biochemical potency (Ki) of 23.3 nM and 72.4 nM against PAK1 and PAK2.