GSK429286A, ROCK1 and ROCK2 inhibitor
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MW 432.4 Da, Purity >98%. Potent, selective, cell-permeable Rho kinase 1 and 2 inhibitor (IC50 values are 14 and 63 nM for ROCK1 and ROCK2 respectively). GSK429286A (ab146581) solution. Blocks cell rounding. Shows antihypertensive effect in vivo. Orally active.
View Alternative Names
70 kDa ribosomal protein S6 kinase 1, 90 kDa ribosomal protein S6 kinase 1, EC 2.7.11.1, HU 1, KIAA0619, KS6A1_HUMAN, KS6B1_HUMAN, MAP kinase-activated protein kinase 1a, MAPK-activated protein kinase 1a, MAPKAP kinase 1a, MAPKAPK-1a, MGC131603, MGC43611, MGC79981, Mitogen-activated protein kinase-activated protein kinase 1A, OTTHUMP00000004113, P70 S6 Kinase, P70 beta 1, PRO0435, PS6K, ROCK-I, ROCK1_HUMAN, ROCK2_HUMAN, ROK alpha, RPS6K1 alpha, RPS6KB1, RSK, RSK 1 p90, RSK-1, Renal carcinoma antigen NY-REN-35, Rho associated coiled coil containing protein kinase 1, Rho associated coiled coil containing protein kinase 2, Rho associated, coiled coil containing protein kinase II, Rho kinase, Rho kinase 2, Rho-alpha kinase, Rho-associated, Rho-associated protein kinase 1, Rho-associated protein kinase 2, Ribosomal S6 kinase 1, Ribosomal protein S6 kinase 70kDa polypeptide 1, Ribosomal protein S6 kinase 90kD 1, Ribosomal protein S6 kinase 90kD polypeptide 1, Ribosomal protein S6 kinase 90kDa polypeptide 1, Ribosomal protein S6 kinase I, Ribosomal protein S6 kinase alpha-1, Ribosomal protein S6 kinase beta-1, Ribosomal protein S6 kinase polypeptide 1, Rock II, Rock2m, Rok, Rps6ka1, S6K, S6K-alpha-1, S6K-beta-1, STK14A, Serine/threonine kinase 14 alpha, Serine/threonine protein kinase 14A, coiled-coil-containing protein kinase 1, coiled-coil-containing protein kinase 2, coiled-coil-containing protein kinase I, dJ590P13.1, dJ590P13.1 (ribosomal protein S6 kinase, 90kD, polypeptide 1, p160 ROCK, p160 ROCK-1, p160 Rhoassociated coiled coil-forming protein kinase, p164 ROCK-2, p70 S6 kinase alpha, p70 S6 kinase, alpha 1, p70 S6 kinase, alpha 2, p70 S6K-alpha, p70 S6KA, p70 S6KB, p70 ribosomal S6 kinase alpha, p70 ribosomal S6 kinase beta 1, p70(S6K)-alpha, p70-S6K, p70-S6K 1, p70-alpha, p90-RSK 1, p90S6K, p90rsk, pp90RSK1, rps6ka
- Chemical Structure
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Chemical Structure - GSK429286A, ROCK1 and ROCK2 inhibitor (AB146581)
2D chemical structure image of ab146581, GSK429286A, ROCK1 and ROCK2 inhibitor
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Supplementary information
This supplementary information is collated from multiple sources and compiled automatically.
Biological function summary
The RSK1 kinase regulates protein synthesis and cell proliferation by phosphorylating various substrates including the ribosomal S6 protein. This kinase connects with the MAPK/ERK signaling pathway and functions as a mediator of cellular response to extracellular signals. S6K1 a downstream effector of mTORC1 is important for protein translation and cell growth. ROCK1 and ROCK2 play key roles in actin cytoskeletal reorganization and are part of the Rho/ROCK complex influencing cell motility shape and apoptosis.
Pathways
RSK1 integrates into the MAPK/ERK pathway where it contributes to the phosphorylation of substrates like CREB and other transcription factors driving gene expression changes. S6K1 aligns with the mTOR pathway where it is vital for the regulation of cellular metabolism and growth. Within the Rho/ROCK pathway ROCK1 and ROCK2 influence the cytoskeleton interfacing with proteins such as LIMK1 and cofilin modulating actin dynamics.
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