[CAS NO. 127191-97-3] KN-62

Name: KN-62
Brand: Arctom Scientific
SKU: SLK-S7422

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PRODUCTS SPECIFICATIONS [127191-97-3]

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Catalog

SLK-S7422

Brand

Selleck

CAS

127191-97-3

DESCRIPTION [127191-97-3]

Overview

MDL	-
Molecular Weight	721.84
Molecular Formula	C38H35N5O6S2
SMILES	S(N([C@H](C(=O)N1CCN(CC1)C2=CC=CC=C2)CC3=CC=C(OS(=O)(=O)C=4C5=C(C=CC4)C=NC=C5)C=C3)C)(=O)(=O)C=6C7=C(C=CC6)C=NC=C7

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.3853 mL	6.9267 mL	13.8535 mL
5 mM	0.2771 mL	1.3853 mL	2.7707 mL
10 mM	0.1385 mL	0.6927 mL	1.3853 mL
50 mM	0.0277 mL	0.1385 mL	0.2771 mL

Description

KN-62 is a potent and specific inhibitor of with of 0.9 μM; also a non-competitive antagonist of the (IC50 = 15 nM). It is selective for CaMKII relative to PKA, PKC and MLCK, but inhibits CaMKI and CaMKIV equally well, The Ki value of KN-62 for CaMK V is 0.8 μM.

Targets

CaMKⅠ ^[5]	CaMKⅣ ^[6]	P2RX7 ^[8]	CaMKⅤ ^[7]	CaMKII ^[1]
			0.8 μM(Ki)	0.9 μM(Ki)

In vitro

KN-62 suppresses the A23187-induced autophosphorylation of Ca2+/CaM kinase in PC12 D cells. KN-62 (10 μM) inhibits carbachol and potassium-stimulated insulin secretion from rat pancreatic islets. KN-62 also inhibits growth of K562 cells and blocks cell cycle progression.

In vivo

KN-62 inhibits seizure-induced expression of brain-derived neurotrophic factor mRNA in adult rat brain.

References

[1] Tokumitsu H, et al. J Biol Chem. 1990, 265(8), 4315-4320.
[2] Wenham RM, et al. Biochem Biophys Res Commun. 1992, 189(1), 128-133.
[3] Minami H, et al. Biochem Biophys Res Commun. 1994, 199(1), 241-248.
[4] Murray KD, et al. Eur J Neurosci. 1998, 10(1), 377-387.
[5] Pellicena P, et al. Front Pharmacol. 2014, 20;5:21.
[6] Enslen H, et al. J Biol Chem. 1994, 269(22):15520-7.
[7] Mochizuki H, et al. J Biol Chem. 1993, 268(12):9143-7.
[8] Chessell IP, et al. Br J Pharmacol. 1998, 124(6):1314-20.

Synonyms

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

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

4-[(2S)-2-[(5-Isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl]phenyl 5-isoquinolinesulfonate

KN 62

[4-[(2S)-2-[Isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxo-3-(4-phenylpiperazin-1-yl)propyl]phenyl] isoquinoline-5-sulfonate