A cell-permeable, pyrrolidine small molecule that promotes single human embryonic stem cell survival up to 20-fold over background (EC50=3.9uM), with equal or higher potency than Y-27632 in 5 cell lines (SA461, SA181, SA167, SA121 and SA002) tested at 10uM. An in vitro high-content screening assay, which profiles a panel of more than 70 protein kinases, indicates that this small molecule is more selective than Y-27632 and only displays an inhibitory effect toward ROCK2 (> 83% inhibition, ROCK1 was not included in the panel) and PRK2 (76% inhibition) at 10uM. Furthermore, it exhibits less cytotoxicity at a greater concentration of 30uM than Y-27632 without marked adverse effects for up to 120 hours.
Molecular Formula:C₁₇H₁₉N₅
Molecular Weight:293.37
Solubility:DMSO (100mg/ml)
Storage and Stability:May be stored at 4°C for short-term only. Aliquot to avoid repeated freezing and thawing. Store at -20°C. Aliquots are stable for 6 months at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
