Y-33075

• CAT Number: I002529
• CAS Number: 199433-58-4
• Molecular Formula: C16H16N4O
• Molecular Weight: 280.32
• Purity: ≥95%
• Synonyms: 4-(1-aminoethyl)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide
• Target: TGF-beta/Smad
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 0.14 uM (Ki) [1]

Y-33075 is potent and selective p160ROCK inhibitor with an Ki value of 0.14 uM, > 200 fold selectivity for p160ROCK than PKC, cAMP-dependent protein kianse and Mypsin light-chain kinase.IC50 value: 0.14 uM (Ki) [1]Target: p160ROCKY-27632 is a representative compound which potently inhibits phenylephrine-induced contraction of rabbit aortic strips, with a half-maximal inhibitory concentration (IC50) of 0.7 uM ; however, it had little effect on contraction induced by potassium chloride (IC50 > 30 uM). Y-27632 also inhibited the contraction of pig coronary artery strips and guinea-pig trachea induced by various agonists such as phenylephrine, histamine, acetylcholine, serotonin, endothelin and a thromboxane agonist, U-46619 (IC50 values of 0.3–1 uM). These results indicate that Y-27632 is a specific and potent inhibitor of agonist-induced smooth-muscle contraction [1].

Reference

[1]. Masayoshi Uehata et al. Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension NATURE | VOL 389 | 30 OCTOBER 199
Abstract
Abnormal smooth-muscle contractility may be a major cause of isease states such as hypertension, and a smooth-muscle relaxant hat modulates this process would be useful therapeutically.Smooth-muscle contraction is regulated by the cytosolic Ca2+ oncentration and by the Ca2+ sensitivity of myo?laments1: the former activates myosin light-chain kinase and the latter is achieved partly by inhibition of myosin phosphatase1 – 3. The small GTPase Rho and its target, Rho-associated kinase, participate in this latter mechanism in vitro 4 – 6, but their participation has not been demonstrated in intact muscles. Here we show that a pyridine derivative, Y-27632, selectively inhibits smooth-muscle contr…