IPA-3 , 10mMinDMSO , 42521-82-4
Synonym(s):
1,1′-Disulfanediyldinaphthalen-2-ol;2,2ʹ-Dihydroxy-1,1ʹ-dinaphthyldisulfide, PAK Inhibitor III;p21-Activated Kinase Inhibitor III, IPA-3 - CAS 42521-82-4 - Calbiochem
Pack Size | Price | Stock | Quantity |
1ml | RMB559.20 | In Stock |
|
others | Enquire |
PRODUCT Properties
Melting point: | 172℃ |
Boiling point: | 543.7±35.0 °C(Predicted) |
Density | 1.46±0.1 g/cm3(Predicted) |
storage temp. | 2-8°C |
solubility | DMSO: >20mg/mL |
pka | 7.52±0.50(Predicted) |
form | Yellow solid |
color | off-white to yellow |
Water Solubility | Soluble in DMSO or ethanol. Insoluble in water. |
Sensitive | Light Sensitive |
Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
CAS DataBase Reference | 42521-82-4 |
Description and Uses
IPA-3 (42521-82-4) is a selective allosteric inhibitor of Group 1 p21-activated kinase (PAK1 IC50?= 2.5 μM)1?via covalent binding to the PAK1 regulatory domain preventing binding to the upstream activator Cdc422. IPA-3 has been shown to induce cell death in human leukemic cell lines3, significantly inhibit TGFβ1-induced prostate cell epithelial to mesenchymal transition4?and inhibit the growth of liver cancer cells5.
p21-activated kinase 1 (PAK1) is a member of a family non-receptor serine/threonine kinases that are vital to normal cell function. Binding of various upstream partners to PAK1 results in release of an autoinhibitory domain that blocks activity of the kinase domain. PAK1 expression and activity is upregulated in several human cancers and is a potential therapeutic target for cancer intervention. IPA-3 is a cell-permeable allosteric inhibitor of PAK1 that is non-competitive with respect to ATP binding (IC50 = 2.5 μM). It does not, however, inhibit the activity of PAK1 that has been pre-activated with Cdc42. IPA-3 binds covalently to the PAK1 regulatory domain (apparent Kd = 1.9 uM) and prevents binding to the upstream activator Cdc42.[Cayman Chemical]
Safety
Symbol(GHS) | GHS05,GHS09 |
Signal word | Danger |
Hazard statements | H318-H410 |
Precautionary statements | P273-P280-P305+P351+P338-P501 |
Hazard Codes | Xi,N |
Risk Statements | 41-50/53 |
Safety Statements | 26-39-60-61 |
RIDADR | UN 3077 9 / PGIII |
WGK Germany | 3 |
HazardClass | 9 |