KN-62

Cas No.:	127191-97-3
Chemical Name:	KN-62
Synonyms:	5-Isoquinolinesulfonicacid,4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl]phenylester;KN-62;(S)-4-(2-(N-Methylisoquinoline-5-sulfonamido)-3-oxo-3-(4-phenylpiperazin-1-yl)propyl)phenyl isoquinoline-5-sulfonate;4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl]phenylisoquinolinesulfonicacidester;5-Isoquinolinesulfonicacid,4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-...;5-Isoquinolinesulfonicacid,4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl]phenyleste;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;1-(N,O-BIS-(5-ISOQUINOLINESULFONYL)-*N-M ETHYL-L-TYR;(S)-4-(2-(N-Methylisoquinoline-5-sulfonaMido)-3-oxo-3-(4-phenylp;1-[N,O-BIS-(5-ISOQUINOLINESULFONYL)-N-METHYL-L-TYROSYL]-4-PHENYLPIPERAZINE;(1-(N,O-BIS-(5-ISOQUINOLINESULFONYL)-N-METHYL-L-TYROSYL)4-PHENYLPIPERAZINE) KN 62;(S)-4-(2-(N-Methylisoquinoline-5-sulfonamido)-3-oxo-3-(4-phenylpiperazin-1-yl)propyl)phenyl is;5-Isoquinolinesulfonic acid 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl]phenyl ester;KN-62 97%;KN-62,97%;KN-62, 99+%;KN-62, >=98%;KN 62;63HM46XPOW;1-(N,O-Bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl)-4-phenylpiperazine;4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl] phenyl isoquinolinesulfonic acid ester;(S)-5-Isoquinolinesulfonic
SMILES:	CN([C@@H](CC1=CC=C(OS(=O)(C2=C3C(C=NC=C3)=CC=C2)=O)C=C1)C(N4CCN(C5=CC=CC=C5)CC4)=O)S(C6=CC=CC7=C6C=CN=C7)(=O)=O
Formula:	C38H35N5O6S2
M.Wt:	721.8444
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	KN-62 is a selective and potent inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with IC50 of 0.9 μM, KN-62 also displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
In Vivo:	The antidepressant-like behavior of ZnCl2 (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 ZnCl2 treatment [F(1,28)=0.84, p>0.05] and a significant effect of KN-62×ZnCl2 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 ZnCl2 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], ZnCl2 treatment [F(1,24)=3.99, p>0.05] and KN-62×ZnCl2 treatment interaction [F(1,24)=0.61, p>0.05])[3].
In Vitro:	KN-62 is a selective antagonist of Ca2+/calmodulin-dependent protein kinase II (CaMKII). KN-62 potently antagonizes ATP-stimulated Ba2+ influx into fura-2 loaded human lymphocytes with an IC50 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 IC50 of 13.1±2.6 nM (n=4) and complete inhibition of the flux at 500 nM[1]. 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 P2X7 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 IC50 of 13.1 nM. KN-62 at a concentration of 3 µM has no effect on ATP-induced ethidium influx through the rat P2X7 receptor, while the IC50 at the human P2X7 receptor is 0.1 µM. KN-62 has considerable selectivity for P2X7 receptors within the P2 family[2].