product name Y-39983 HCl
Description: Y-39983 is a potent and selective inhibitor of Rho-associated coiled coil-forming protein kinase( ROCK ) with IC50 values of 3.6nM, 0.42μM and 0.81μM for ROCK, PKC and CaMKII, respectively. Apart from these, Y-39983 has been reported to relax the ciliary arteries of precontracted isolated rabbit in vitro. In addition, Y-39983 has been found to increase optic-nerve-head blood flow by laser speckle flowmetry. Moreover, Y-39983 lowered the intraocular pressure ( IOP) in a dose-dependent fashion in the eyes of rabbits and monkeys.
References: Nature. 1997 Oct 30;389(6654):990-4; Nat Med. 1999 Feb;5(2):221-5.
320.26
Formula
C14H21N3O.2HCl
CAS No.
129830-38-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 64 mg/mL (199.8 mM)
Water: 14 mg/mL (43.71 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Y-27632 2HCl inhibits ROCK-II while displaying little activity against PKC, cAMP-dependent protein kinase and myosin light-chain kinase (MLCK) with Ki of 26 μM, 25 μM and > 250 μM, respectively, as well as PKA activated by another Rho-family GTPase member, Cdc42. Y-27632 2HCl inhibits smooth-muscle contraction induces by various agonists including phenylephrine, histamine, acetylcholine, serotonin, endothelin, and thromboxane with IC50 of 0.3-1 μM, by selectively inhibiting Ca2+ sensitization. Y-27632 2HCl suppresses Rho-induced, p160ROCK-mediated formation of stress fibres in cultured cells. Y-27632 2HCl treatment blocks both Rho-mediated activation of actomyosin and LPA-stimulated invasive activity of MM1 cells in a concentration-dependent manner. Y-27632 2HCl treatment is not only sufficient to initiate formation of exuberant axonal processes but also facilitates axonal maturation during the very early stages of axonogenesis, while largely sparing axon elongation. In human embryonic stem (hES) cells, Y-27632 2HCl treatment at 10 μM markedly diminishes dissociation-induced apoptosis even in serum-free suspension (SFEB) culture, increases cloning efficiency (from ~1% to ~27%), facilitates subcloning after gene transfer, and enables SFEB-cultured hES cells to survive and differentiate into Bf1+ cortical and basal telencephalic progenitors. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Oral administration of Y-27632 2HCl at 30 mg/kg significantly decreases the blood pressure in a dose-dependent manner in spontaneous hypertensive rats, renal hypertensive rats, as well as deoxycorticosterone acetate (DOCA)-salt hypertensive rats. When Y-27632 2HCl is continuously administered at a rate of 0.55 μL per hour by implanted pumps for 11 days tumor cell invasion (MM1 cells expressing Val14-RhoA in rats) is significantly delayed. By inhibiting ROCK, Y-27632 2HCl treatment attenuates hypoxia-induced angiogenesis and vascular remodeling in the pulmonary circulation. Pretreatment with Y-27632 has a protective effect against tumor formation in albino mice with Ehrlich ascites carcinoma. |
| Animal model | Male Wistar rats with spontaneous or induced hypertension; Swiss albino mice with Ehrlich ascites carcinoma |
| Formulation & Dosage | Dissolved in DMSO, and diluted in saline (Rat); 0.9% NaCl (Mice); 30 mg/kg/day (Rat); 0-10 mg/kg (mice); Orally (Rat); i.p. (Mice) |
| References | Nature. 1997 Oct 30;389(6654):990-4; Nat Med. 1999 Feb;5(2):221-5. |
