Cat. No. 5190
Chemical Name: 6-(2,4-Dichlorophenyl)-8-ethyl-2-[[
Biological ActivityPotent p21-activated kinase (PAK) inhibitor (IC50 values are 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively). Blocks and reverses the DISC1 knockdown-induced reduction in dendritic spine size in cortical neurons. Attenuates dendritic spine elimination and enhances spine generation in DISC1 knockdown mice. Ameliorates autism-like behavioral symptoms in fragile X mental retardation 1 (Fmr1) knockout mice. Brain penetrant and orally bioavailable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Wang et al (2016) P21-activated kinase inhibitors FRAX486 and IPA3: inhibition of prostate stromal cell growth and effects on smooth muscle contraction in the human prostate. PLoS One 11 e0153312. PMID: 27071060.
Dolan et al (2013) Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. Proc.Natl.Acad.Sci.U.S.A. 110 5671. PMID: 23509247.
Hayashi-Takagi et al (2013) PAKs inhibitors ameliorate schizophrenia-associated dendritic spine deterioration in vitro and in vivo during late adolescence. Proc.Natl.Acad.Sci.U.S.A. 111 6461. PMID: 24706880.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products. Selected citations for FRAX 486 include:
Wang et al (2016) P21-activated kinase inhibitors FRAX486 and IPA3: inhibition of prostate stromal cell growth and effects on smooth muscle contraction in the human prostate. PloS One 11 e0153312. PMID: 27071060.
Do you know of a great paper that uses FRAX 486 from Tocris? If so please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: FRAX 486, supplier, FRAX486, potent, p21, activated, kinase, PAK, inhibitors, inhibits, neuroprotective, brain, penetrant, orally, bioavailable, Tocris Bioscience, P21-activated Kinases Inhibitor products
Find multiple products by catalog number
New Products in this Area
Potent and selective PFKFB3 inhibitorSTOCK2S 26016
Lysine deficient protein kinase (WNK) signaling inhibitorrac-CCT 250863
Potent Nek2 inhibitorRoscovitine
Potent, selective cyclin-dependent kinase inhibitorEnzastaurin
Potent PKCβ inhibitorBMS 265246
Potent cdk1/2 inhibitorAutocamtide-2-related inhibitory peptide, myristoylated
CaM kinase II inhibitor; enhanced cell permeable derivative of Autocamtide-2-related inhibitory peptideMP A08
Selective ATP competitive SphK1 and 2 inhibitor; cell permeableAkti-1/2
Potent and selective dual Akt1 and 2 inhibitorVX 680
High affinity and selective Aurora kinase inhibitorImatinib mesylate
Potent and selective v-Abl tyrosine kinase inhibitor; also inhibits PDGFR and c-kitTGX 221
Potent and selective PI 3-kinase β inhibitorPF 543 hydrochloride
Potent and selective SphK1 inhibitorJX 06
Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3 inhibitorMRT 68601 hydrochloride
Potent TBK1 inhibitor
Follow Tocris on LinkedIn
Visit our LinkedIn page for the latest Tocris news, events and updates.