Y-39983

Additional information:
Y-39983 (free base), also known as Y-33075, is a potent and selective inhibitor of ROCK family with IC50 value of 3.6nM for ROCK. Y-39983 attenuates experimental autoimmune encephalomyelitis via inhibition of demyelination. Y-39983 downregulates RhoA/Rho-associated kinase expression during its promotion of axonal regeneration. Y-39983, promotes regeneration of crushed axons of retinal ganglion cells into the optic nerve of adult cats.|Product information|CAS Number: 199433-58-4|Molecular Weight: 280.32|Formula: C16H16N4O|Synonym:|Y33075|Chemical Name: (R)-4-(1-aminoethyl)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide|Smiles: C[C@@H](N)C1C=CC(=CC=1)C(=O)NC1C=CN=C2NC=CC=12|InChiKey: JTVBXQAYBIJXRP-SNVBAGLBSA-N|InChi: InChI=1S/C16H16N4O/c1-10(17)11-2-4-12(5-3-11)16(21)20-14-7-9-19-15-13(14)6-8-18-15/h2-10H,17H2,1H3,(H2,18,19,20,21)/t10-/m1/s1|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|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.{{Mucicarmine} MedChemExpress|{Mucicarmine} {Fluorescent Dye}|{Mucicarmine} Biological Activity|{Mucicarmine} Purity|{Mucicarmine} supplier|{Mucicarmine} Cancer} Y-33075 (10 μM) shows no effect on the [Ca2+]i increase with the high-potassium (high-K) solution.{{Simeprevir} medchemexpress|{Simeprevir} HCV|{Simeprevir} Protocol|{Simeprevir} In Vitro|{Simeprevir} manufacturer|{Simeprevir} Autophagy} |In Vivo:|In rabbits, Y-39983 (≥0.PMID:35901518 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.|References:|Inoue T, Tanihara H, Tokushige H, Araie M. Efficacy and safety of SNJ-1656 in primary open-angle glaucoma or ocular hypertension. Acta Ophthalmol. 2015 Aug;93(5):e393-5. doi: 10.1111/aos.12641. Epub 2015 Mar 17. PubMed PMID: 25783615.Chen KG, Hamilton RS, Robey PG, Mallon BS. Alternative cultures for human pluripotent stem cell production, maintenance, and genetic analysis. J Vis Exp. 2014 Jul 24;(89). doi: 10.3791/51519. PubMed PMID: 25077932; PubMed Central PMCID: PMC4206262.Van de Velde S, Van Bergen T, Sijnave D, Hollanders K, Castermans K, Defert O, Leysen D, Vandewalle E, Moons L, Stalmans I. AMA0076, a novel, locally acting Rho kinase inhibitor, potently lowers intraocular pressure in New Zealand white rabbits with minimal hyperemia. Invest Ophthalmol Vis Sci. 2014 Feb 18;55(2):1006-16. doi: 10.1167/iovs.13-13157. PubMed PMID: 24474276.Products are for research use only. Not for human use.|