GSK429286A, 10 mg

A research-use small molecule from STEMCELL Technologies, this compound is a cell-permeable inhibitor of Rho-associated kinases ROCK1 and ROCK2, with IC₅₀ values of 14 and 63 nM, respectively. It also shows selectivity towards p90 and p70 ribosomal S6 kinases (RSK) and leucine-rich repeat kinase-2 (LRRK2), with IC₅₀ values in the high nanomolar range, and is reported to have improved oral bioavailability compared to closely related inhibitors.

The chemical name is N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide, with CAS number 864082-47-3, alternative name GSK 429286, molecular formula C₂₁H₁₆F₄N₄O₂, and molecular weight of 432.4 g/mol. Purity is reported as ≥ 98%. It is supplied as a crystalline solid with reported solubility of ~0.5 mg/mL in 1:1 DMSO:PBS (pH 7.2), ~1 mg/mL in EtOH, and ~10 mg/mL in DMSO and DMF. The manufacturer recommends storage at -20°C, protected from prolonged exposure to light.

Published applications include inducing senescence-resistant proliferation of keratinocytes, supporting survival and cloning efficiency of dissociated human pluripotent stem cells (when used as part of the ROCK inhibitor class), reversing adrenalin-induced contraction of rat aortic tissue, and decreasing mean arterial pressure in spontaneously hypertensive rats. According to the manufacturer's Safety Data Sheet, the compound is classified as Acute Toxicity, Oral, Category 3 (H301: Toxic if swallowed) and should be handled with appropriate laboratory chemical safety practices, including compatible chemical-resistant gloves, lab coat, safety glasses, and respiratory protection as warranted.