| 应用 |
A potent and selective inhibitor of CaMKII |
| 产品介绍 |
KN-62是可渗透入细胞的CaM激酶II抑制剂，IC50为0.9 μM，直接与该酶的钙调蛋白结合位点结合，同时还是非竞争性P2X7受体拮抗剂，IC50为15 nM。 |
| 生化机理 |
KN-62 has demonstrated potent and selective inhibition of Ca2+/calmodulin-dependent protein kinase II (CaMKII; Ki=0.9 μM) which causes cells to arrest in the S phase. In HEK-293 cells expressing type III adenylyl cyclase (III-AC), 10 μM of KN-62 blocked CaMKII phosphorylation of III-AC, and inhibited hormone-stimulated Ca2+ oscillations. Additionally, KN-62 is a potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM). |
| 别名 |
KN 62; KN62;5-异喹啉磺酸 4-[(2S)-2-[(5-异喹啉磺酰基)甲氨基]-3-氧代-3-(4-苯基-1-哌嗪基)丙基]苯酯;KN 62; KN62; (S)-5-Isoquinolinesulfonic acid 4-[2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl]phenyl ester; 1-[N,O-bis(5-Isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine |
