KN-62

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KN-62 是 Ca2+/钙调蛋白依赖性蛋白激酶 II (CaMK II) 的特异性抑制剂，对大鼠脑 CaMK II 的 Ki 为 900 nM。

KN-62 is a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMK II) with Ki of 900 nM for rat brain CaMK II; potently antagonizes ATP-stimulated Ba2+ influx into fura-2 loaded human lymphocytes with IC50 of 12.7 nM, inhibits ATP-stimulated ethidium+ uptake with IC50 of 13.1 nM; causes hypertension and tachycardia in rats, associated with the diminished rate of GABA release in cerebrospinal fluid.

KN-62 potently antagonizes ATP-stimulated Ba2+ influx into fura-2 loaded human lymphocytes with an IC50 of 12.7 nM and complete inhibition of the flux at a concentration of 500 nM. KN-62 does not inhibit the activity of autophosphorylated Ca2+/CaM kinase II. KN-62 inhibits the Ca2+/calmodulin-dependent autophosphorylation of both alpha (50 kDa) and beta (60 kDa) subunits of Ca2+/CaM kinase II dose dependently in the presence or absence of exogenous substrate. 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 IC50 of 13.1 nM.

KN62 (5mg/kg/day; ip; three times a week for 6 weeks) significantly reduces the liver metastatic tumor burden in five weeks old BALB/c athymic nude mice inoculated with TAMR-MCF-7 cells. ?KN-62 (1 μg/site, i.c.v.) prevents the antidepressant-like behavior and antidepressant-like behaviors of ZnCl2 (10 mg/kg, p.o.).

KN 62 | KN62

Endocrinology/Hormones

CaMK

CaMKⅤ|CaMKII

Metabolic Disease

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127191-97-3

721.9

C38H35N5O6S2

>98% (HPLC)

10 mM in DMSO

CN(C(CC1=CC=C(C=C1)OS(=O)(=O)C2=CC=CC3=C2C=CN=C3)C(=O)N4CCN(CC4)C5=CC=CC=C5)S(=O)(=O)C6=CC=CC7=C6C=CN=C7

5-Isoquinolinesulfonic acid, 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl]phenyl ester

(-20℃)

With Ice Pack

≥ 2 years