KN-62, Thermo Scientific Chemicals

Potently and specifically inhibits calcium/calmodulin kinase II

It is used as a potent and selective inhibitor of CaMKII. KN-62 has demonstrated potent and selective inhibition of Ca2+/calmodulin-dependent protein kinase II (CaMKII; Ki=0.9 ?M) which causes cells to arrest in the S phase. In HEK-293 cells expressing type III adenylyl cyclase (III-AC), 10 ?M 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).

This Thermo Scientific Chemicals brand product was originally part of the Alfa Aesar product portfolio. Some documentation and label information may refer to the legacy brand. The original Alfa Aesar product / item code or SKU reference has not changed as a part of the brand transition to Thermo Scientific Chemicals.

Applications
It is used as a potent and selective inhibitor of CaMKII. 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).

Solubility
Soluble in 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin (0.93 mg/ml), methanol (10 mg/ml), DMSO (12 mg/ml), chloroform (20 mg/ml), ethanol (∼1 mg/ml), 1:2 DMF:PBS (pH 7.2) (∼0.3 mg/ml), and DMF & DMSO (∼30 mg/ml).

Notes
Store in cool place. Keep container tightly closed in a dry and well-ventilated place. Recommended storage temperature: -20°C. Keep away from strong oxidizing agents.

Chemical Identifiers

CAS

127191-97-3

Molecular Formula

C38H35N5O6S2

Molecular Weight (g/mol)

721.85

MDL Number

MFCD00083180

InChI Key

RJVLFQBBRSMWHX-UHFFFAOYNA-N

Synonym

s-4-2-n-methylisoquinoline-5-sulfonamido-3-oxo-3-4-phenylpiperazin-1-yl propyl phenyl isoquinoline-5-sulfonate, unii-63hm46xpow, chembl28324, 63hm46xpow, 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, 4-2s-2-5-isoquinolinylsulfonyl methylamino-3-oxo-3-4-phenyl-1-piperazinyl propyl phenyl isoquinolinesulfonic acid ester, 4-2s-2-n-methylisoquinoline-5-sulfonamido-3-oxo-3-4-phenylpiperazin-1-yl propyl phenyl isoquinoline-5-sulfonate, 5-isoquinolinesulfonic acid, 4-2s-2-5-isoquinolinylsulfonyl methylamino-3-oxo-3-4-phenyl-1-piperazinyl propyl phenyl ester

PubChem CID

5312126

IUPAC Name

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

SMILES

CN(C(CC1=CC=C(OS(=O)(=O)C2=C3C=CN=CC3=CC=C2)C=C1)C(=O)N1CCN(CC1)C1=CC=CC=C1)S(=O)(=O)C1=C2C=CN=CC2=CC=C1

Melting Point

65°C to 67°C

Color

Yellow

Linear Formula

NH₂(CH₂)₁₀NH₂

Quantity

1 mg

Solubility Information

Soluble in 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin (0.93mg/ml),methanol (10mg/ml),DMSO (12mg/ml),chloroform (20mg/ml),ethanol (∽1mg/ml),1:2 DMF:PBS (pH 7.2) (∽0.3mg/ml),and DMF & DMSO (∽30mg/ml).

Formula Weight

721.84

Physical Form

Powder

Chemical Name or Material

KN-62

TSCA

No

Recommended Storage

Store at -20°C

SDS

TSCA

No

Recommended Storage

Store at -20°C

SDS

RUO – Research Use Only