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Y-33075
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Y-33075
CAS No. : 199433-58-4
MCE 站:Y-33075
产品活性:Y-33075 是一种有效的 ROCK 抑制剂,源于 Y-27632,但活性更强,IC50 值 3.6 nM。
研究领域:Cell Cycle/DNA Damage | Stem Cell/Wnt | Cytoskeleton | TGF-beta/Smad
作用靶点:ROCK
In Vitro: Y-33075 (Y-39983) is a potent ROCK inhibitor, with an IC50 of 3.6 nM. Y-33075 also inhibits PKC and CaMKII more potently than Y-27632, and the IC50s of Y-27632 and Y-33075 for PKC are 9.0 μM and 0.42 μM, respectively, whereas the IC50s of Y-27632 and Y-33075 for CaMKII are 26 μM and 0.81 μM, respectively. The IC50s of Y-27632 and Y-33075 for PKC is 82 and 117 times those for ROCK, respectively, whereas the IC50s of Y-27632 and Y-33075 for CaMKII is 236 and 225 times those for ROCK, respectively. Y-33075 (Y-39983, 10 μM) extends neurites in the retinal ganglion cells (RGCs) compared with those in RGCs treated without Y-39983. Y-33075 (Y-39983, 1 μM) inhibits the contraction of rabbit ciliary artery segments evoked by histamine in Ca2+-free solutions. Y-33075 (10 μM) shows no effect on the [Ca2+]i increase with the high-potassium (high-K) solution.
In Vivo: In rabbits, Y-39983 (≥0.01%) significantly lowers intraocular pressure (IOP) at 2 hours after topical administration. In monkeys, Y-39983 (0.05%)-treated eyes show significant reduction of IOP between 2 and 7 hours after topical administration. Y-39983 (100 μM) increases the regenerating axons of retinal ganglion cells (RGCs) in the eyes of the rats.
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Stem Cell Signaling Compound Library | TGF-beta/Smad Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Reprogramming Compound Library | Cytoskeleton Compound Library | Y-27632 dihydrochloride | Chroman 1 | Fasudil Hydrochloride | Narciclasine | Ripasudil | GSK429286A | CMPD101 | H-1152 dihydrochloride | Y-33075 dihydrochloride | Hydroxyfasudil | BDP5290 | SR-3677 | SB-772077B dihydrochloride | Pentanoic acid | ZINC00881524 | Verosudil | ROCK-IN-1 | ROCK2-IN-2
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