IPA-3 - CAS 42521-82-4
Catalog number:
Not Intended for Therapeutic Use. For research use only.
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Molecular Weight:
p21-activated Kinases (PAKs)
IPA-3 is a selective non-ATP competitive Pak1 inhibitor with IC50 of 2.5 μM, no inhibition to group II PAKs (PAKs 4-6).
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1.Liposomal-mediated delivery of the p21 activated kinase-1 (PAK-1) inhibitor IPA-3 limits prostate tumor growth in vivo.
Al-Azayzih A1, Missaoui WN2, Cummings BS3, Somanath PR4. Nanomedicine. 2016 Mar 3. pii: S1549-9634(16)00073-3. doi: 10.1016/j.nano.2016.01.003. [Epub ahead of print]
P21 activated kinases-1 (PAK-1) is implicated in various diseases. It is inhibited by the small molecule 'inhibitor targeting PAK1 activation-3' (IPA-3), which is highly specific but metabolically unstable. To address this limitation we encapsulated IPA-3 in sterically stabilized liposomes (SSL). SSL-IPA-3 averaged 139nm in diameter, polydispersity index (PDI) of 0.05, and a zeta potential of -28.1, neither of which changed over 14days; however, the PDI increased to 0.139. Analysis of liposomal IPA-3 levels demonstrated good stability, with 70% of IPA-3 remaining after 7days. SSL-IPA-3 inhibited prostate cancer cell growth in vitro with comparable efficacy to free IPA-3. Excitingly, only a 2day/week dose of SSL-IPA-3 was needed to inhibit the growth of prostate xenografts in vivo, while a similar dose of free IPA-3 was ineffective. These data demonstrate the development and clinical utility of a novel liposomal formulation for the treatment of prostate cancer.
2.Inhibition of p21-activated Kinase 1 by IPA-3 Promotes Locomotor Recovery after Spinal Cord Injury in Mice.
Ji X1, Zhang Y, Zhang L, Chen H, Peng Y, Tang P. Spine (Phila Pa 1976). 2016 Feb 6. [Epub ahead of print]
STUDY DESIGN: Ninety-six male adult CD-1 mice were randomly divided into sham, SCI + Vehicle and SCI + IPA-3 groups. Expression of matrix metalloproteinase (MMP)-2 and MMP-9, production of TNF-α and IL-1β, tissue edema, blood-spinal cord barrier (BSCB) penetrability, neural cell apoptosis, and neurological function recovery were measured.
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