Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 2038-03-1, Name is 2-Morpholinoethanamine, molecular formula is , belongs to isoquinoline compound. In a document, author is Lu, ZX, Recommanded Product: 2038-03-1.
Selective inhibition of cyclic AMP-dependent protein kinase by isoquinoline derivatives
A large series of isoquinoline derivatives was synthesised including derivatives of isoquinoline, isoquinolino[3,4-c]furazan, 1,2-dihydro-1-oxoisoquinoline, 6-oxopyrimido[1 ,2-b]isoquinoline, benzo[c][1,8]-naphthyridine, pyrazino[2,3-c]isoquinoline and benzimidazoe[2,1 -a]isoquinoline as well as further structurally related isoquinoline derivatives and pyrido-2,3-furazans. Representatives of all of these classes of isoquinolines are potent and selective inhibitors of the cyclic AMP-dependent protein kinase (PKA) catalytic subunit (cAK) from rat liver, The most effective cAK inhibitors are a series of 1,3-di-substituted and 1,3,4-tri-substituted isoquinolines (IC50 values 30 – 50 nM) (compounds A1, A2, A3, A4 and A5) and 2-ethylcarboxy-3-amino-5,6-dihydro-6-oxobenzo[c] [1 8]naphthyridine (El) (IC50 0.08 mu M) Compounds A1-A5 inhibit cAK in a fashion that is competitive with respect to ATP as substrate, The isoquinoline inhibitors A1-A5 are ineffective or very poor inhibitors of wheat embryo Ca2+-dependent protein kinase (CDPK) and rat brain Ca2+-dependent protein kinase C (PKC), chicken gizzard myosin light chain kinase (MLCK) and potato tuber cyclic nucleotide-binding phosphatase (Pase), E1 is a moderately effective inhibitor of CDPK and PKC (IC50 values 30 and 61 mu M, respectively), The bisisoquinoline-1 (2H)-one compound B7 inhibits cAK, CDPK, PKC and MLCK (IC50 values 8, 95, 24 and 7 mu M, respectively) as does J1 [2-(p-bromophenyl)pyrrolo[2,3-c]isoquinoline-5(4H)-one] (IC50 values 2, 50, 44 and 7 mu M, respectively), The very potent isoquinoline-derived cAK inhibitors found here involve substitution of the N-containing isoquinoline ring system and these inhibitors show high specificity for cAK.
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Reference:
Isoquinoline – Wikipedia,
,Isoquinoline | C9H7N – PubChem