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GSK429286A

RHO/ROCK pathway inhibitor; Inhibits ROCK1 and ROCK2

STEMCELL Technologies Inc.

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GSK429286A is a cell-permeable inhibitor of Rho-associated kinases ROCK1 and ROCK2 with IC₅₀ values of 14 and 63 nM, respectively. It has improved oral bioavailability compared to closely related inhibitors. It also shows some selectivity towards p90 and p70 ribosomal S6 kinases (RSK) and leucine-rich repeat protein kinase-2 (LRRK2), with IC₅₀ values in the high nanomolar range (Goodman et al.; Nichols et al.).

MAINTENANCE

  • Induces senescence-resistant proliferation of keratinocytes (Chapman et al.).
  • ROCK inhibitors such as Y-27632 enhance the survival and cloning efficiency of human pluripotent stem cells when they are dissociated to single cells (Watanabe et al.)

DISEASE MODELING

  • Reverses adrenalin-induced contraction of rat aortic tissue and decreases mean arterial pressure in spontaneously-hypertensive rats (Goodman et al.).

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