Pro-survival Compound, DDD00033325-Calbiochem

C₁₇H₁₉N₅

293.37

A cell-permeable, pyrrolidine small molecule that promotes single human embryonic stem cell survival up to 20-fold over background (EC₅₀ = 3.9 M), with equal or higher potency than Y-27632 in 5 cell lines (SA461, SA181, SA167, SA121 and SA002) tested at 10 M. 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 10 M. Furthermore, it exhibits less cytotoxicity at a greater concentration of 30 M than Y-27632 without marked adverse effects for up to 120 hours.
A cell-permeable, pyrrolidine small molecule that promotes single human embryonic stem cell survival up to 20-fold over background (EC₅₀ = 3.9 M), with equal or higher potency than Y-27632 (Cat. No. 688000) in 5 cell lines (SA461, SA181, SA167, SA121 and SA002) tested at 10 M. 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 10 M. Furthermore, it exhibits less cytotoxicity at a greater concentration of 30 M than Y-27632 without marked adverse effects for up to 120 hours.

Toxicity: Regulatory Review (Z)

Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 3 months at -20°C.

Andrews, P.D., et al. 2010. Biochem. J.432, 21.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥95% (HPLC)

syrup

Calbiochem^®

OK to freeze
protect from light

yellow

DMSO: 100 mg/mL

wet ice

−20℃

C12=CC=NN1C=CC(N[C@@H]3CCN(CC4=CC=CC=C4)C3)=N2

10 mg in Glass bottle
Packaged under inert gas

10 - Combustible liquids

WGK 1