1-[N,O-二(5-异喹啉磺酰基)-N-甲基-L-型酪氨酸]-4-苯基哌嗪 CAS#: 127191-97-3

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1-[N,O-二(5-异喹啉磺酰基)-N-甲基-L-型酪氨酸]-4-苯基哌嗪

生物活性靶点体外研究体内研究 用途与合成方法 MSDS 1-[N,O-二(5-异喹啉磺酰基)-N-甲基-L-型酪氨酸]-4-苯基哌嗪价格(试剂级) 上下游产品信息

中文名称	1-[N,O-二(5-异喹啉磺酰基)-N-甲基-L-型酪氨酸]-4-苯基哌嗪
中文同义词	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;1-[N,O-二(5-异喹啉磺酰基)-N-甲基-L-型酪氨酸]-4-苯基哌嗪;化合物KN-62;(S)-4-(2-(N-甲基异喹啉-5-磺胺)-3-氧代-3-(4-苯基哌嗪-1-基)丙基)苯基异喹啉-5-磺酸盐;KN-62,CAM激酶II抑制剂;4-[(2S)-2-[(5-异喹啉基磺酰基)甲氨基]-3-OXO-3-(4-苯基-1-哌嗪基)丙基]苯基异喹啉磺酸酯
英文名称	KN-62
英文同义词	1-(N,O-BIS-(5-ISOQUINOLINESULFONYL)-*N-M ETHYL-L-TYR;KN-62 97%;KN-62, 99+%;4-((2S)-2-((5-isoquinolinylsulfonyl)methylamino)-3-oxo-3-(4-phenyl-1-piperazinyl)propyl)phenylisoquinolinesulfonicacid;1-(N,O-Bis-[5-isoquinolinesulfonyl]-N-methyl-L-tyrosyl)-4-phenylpiperazine, (S)-5-Isoquinolinesulfonic Acid 4-(2-[(5-Isoquinolinylsulfonyl)methylamino]- 3-oxo-3-[4-phenyl-1-piperazinyl]propyl)phenyl Ester,;5-Isoquinolinesulfonic acid, 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl]phenyl ester;(s)-5-isoquinolinesulfonic acid 4-[2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl]phenyl ester;CS-756
CAS号	127191-97-3
分子式	C38H35N5O6S2
分子量	721.84
EINECS号
相关类别	定制化学品;库存;Inhibitor;Protein Kinase;Protein Kinase Inhibitors and Activators
Mol文件	127191-97-3.mol
结构式

1-[N,O-二(5-异喹啉磺酰基)-N-甲基-L-型酪氨酸]-4-苯基哌嗪 性质

1-[N,O-二(5-异喹啉磺酰基)-N-甲基-L-型酪氨酸]-4-苯基哌嗪 用途与合成方法

生物活性

KN-62 是一种有效，选择性的钙调蛋白依赖性蛋白激酶 II (CaMK-II)抑制剂，IC50 为 0.9 μM， KN-62 也是非竞争性的 P2X7 受体拮抗剂，IC50 约为 15 nM。

靶点

IC50: 0.9 μM (CaMK II), 15 nM (P2X     ₇    receptor, in HEK293 cells)

体外研究

KN-62 is a selective antagonist of Ca     ²⁺    /calmodulin-dependent protein kinase II (CaMKII). KN-62 potently antagonizes ATP-stimulated Ba     ²⁺    influx into fura-2 loaded human lymphocytes with an IC     ₅₀    of 12.7±1.5 nM (n=3) and complete inhibition of the flux at a concentration of 500 nM. Similarly, KN-62 inhibits ATP-stimulated ethidium     ⁺    uptake, measured by time resolved flow cytometry, with an IC     ₅₀    of 13.1±2.6 nM (n=4) and complete inhibition of the flux at 500 nM. KN-62 is found to be a potent antagonist in a functional assay, inhibition of ATP-induced K     ⁺    efflux in HEK293 cells expressing recombinant human P2X     ₇    receptors. In human leukemic B lymphocytes, KN-62 reduces the rate of permeability increase to larger permeant cations, like ethidium, induced by Bz-ATP with an IC     ₅₀    of 13.1 nM. KN-62 at a concentration of 3 µM has no effect on ATP-induced ethidium influx through the rat P2X     ₇    receptor, while the IC     ₅₀    at the human P2X     ₇    receptor is 0.1 µM. KN-62 has considerable selectivity for P2X     ₇    receptors within the P2 family.

体内研究

The antidepressant-like behavior of ZnCl     ₂    (10 mg/kg, p.o.) (p<0.01) is prevented by CAMKII inhibitor KN-62 (1 μg/site, i.c.v.). The two-way ANOVA reveals a significantly main effect of KN-62 treatment [F(1,28)=27.47, p<0.01], no main effect of ZnCl  ₂    treatment [F(1,28)=0.84, p>0.05] and a significant effect of KN-62×ZnCl     ₂    treatment interaction [F(1,28)=22.57, p<0.01] to immobility time. As revealed by the post-hoc analysis, the anti-immobility effect of ZnCl  ₂    is completely prevented by treatment of animals with KN-62. No effect in locomotor activity in the open-field test is observed: (KN-62 treatment [F(1,24)=1.97, p>0.05], ZnCl     ₂    treatment [F(1,24)=3.99, p>0.05] and KN-62×ZnCl     ₂    treatment interaction [F(1,24)=0.61, p>0.05]).

安全信息

MSDS信息

1-[N,O-二(5-异喹啉磺酰基)-N-甲基-L-型酪氨酸]-4-苯基哌嗪 价格(试剂级)

1-[N,O-二(5-异喹啉磺酰基)-N-甲基-L-型酪氨酸]-4-苯基哌嗪 上下游产品信息