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Y-33075

Catalog No. T13384 CAS 199433-58-4

Synonyms: Y 39983

Y-33075 is a selective inhibitor of ROCK derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.

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Y-33075, CAS 199433-58-4

Pack Size	Availability	Price/USD
2 mg	5 days	$ 112.00
25 mg	6-8 weeks	$ 766.00
50 mg	6-8 weeks	$ 995.00
100 mg	6-8 weeks	$ 1,630.00
1 mL * 10 mM (in DMSO)	5 days	$ 329.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Y-33075 is a selective inhibitor of ROCK derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.
Targets&IC50	PKC:420 nM, ROCK:3.6 nM, CaMK II:810 nM
In vitro	Y-33075 (Y-39983) is a potent inhibitor of ROCK(IC50 of 3.6 nM). Y-33075 also inhibits PKC and CaMKII more potently than Y-27632(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[1]. Y-33075 (Y-39983, 10 μM) extends neurites in the retinal ganglion cells (RGCs) compared with those in RGCs treated without Y-39983[2]. Y-33075 (Y-39983, 1 μM) inhibits the contraction of rabbit ciliary artery segments evoked by histamine in Ca2+-free solutions[3].
In vivo	Y-39983, when administered topically at concentrations of 0.01% or higher, significantly reduces intraocular pressure (IOP) in rabbits within 2 hours. In monkeys, eyes treated with 0.05% Y-39983 demonstrate a substantial decrease in IOP from 2 to 7 hours post-administration. Additionally, at a concentration of 100 μM, Y-39983 fosters the growth of regenerating axons in the retinal ganglion cells (RGCs) of rats.

Synonyms	Y 39983
Molecular Weight	280.32
Formula	C16H16N4O
CAS No.	199433-58-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (178.37 mM), Sonification and heating are recommended.

References and Literature

1. Hideki Tokushige, et al. Effects of Topical Administration of Y-39983, a Selective Rho-Associated Protein Kinase Inhibitor, on Ocular Tissues in Rabbits and Monkeys Invest. Ophthalmol. Vis. Sci. July 2007 vol. 48no. 7 3216-3222 2. Tokushige H, et al. Effects of Y-39983, a selective Rho-associated protein kinase inhibitor, on blood flow in optic nerve head in rabbits and axonal regeneration of retinal ganglion cells in rats. Curr Eye Res. 2011 Oct;36(10):964-70. 3. Watabe H, et al. Effects of Rho-associated protein kinase inhibitors Y-27632 and Y-39983 on isolated rabbit ciliary arteries.Jpn J Ophthalmol. 2011 Jul;55(4):411-7. Epub 2011 Jun 11.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Y-33075 199433-58-4 Chromatin/Epigenetic Cytoskeletal Signaling PKC Y 39983 Y33075 Y-39983 Y39983 Y 33075 inhibitor inhibit

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