Chemical Name: 8-[(trans-5-Amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-pyrido[2,3-d]pyrimidin-7(8H)-one
Biological ActivityG 5555 is a high affinity group 1 PAK (pan-PAK1, 2 and 3) inhibitor (Ki = 3.7 nM; pMEK IC50 = 69 nM). Of 235 kinases tested, other than PAK1, eight (PAK2, PAK3, KHS1, Lck, MST3, MST4, SIK2, and YSK1) were inhibited >70%. Exhibits low hERG channel activity (<50% inhibition at 10 μM). Orally bioavailable.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Complete Your Research
Design of selective PAK1 inhibitor G-5555: improving properties by employing an unorthodox low-pK a polar moiety.
Ndubaku et al.
ACS Med.Chem.Lett., 2015;6:1241
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