422708

KN-93

A cell-permeable, reversible and competitive inhibitor of rat brain CaM kinase II (K_i = 370 nM).

• Synonym(s): 2-[N-(2-hydroxyethyl)]-N-(4-methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine)
• Empirical Formula (Hill Notation): C₂₆H₂₉ClN₂O₄S
• CAS Number: 139298-40-1
• Molecular Weight: 501.04
• MDL number: MFCD03788201

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C26H29ClN2O4S/c1-28(17-5-6-21-9-11-23(27)12-10-21)20-22-7-3-4-8-26(22)29(18-19-30)34(31,32)25-15-13-24(33-2)14-16-25/h3-16,30H,17-20H2,1-2H3/b6-5+
• InChI key: LLLQTDSSHZREGW-AATRIKPKSA-N

Description

General description

A cell-permeable, reversible and competitive inhibitor of rat brain CaM kinase II (K_i = 370 nM). Selectively binds to the CaM binding site of the enzyme and prevents the association of CaM with CaMKII. Has no significant effects on protein kinase A activity. Induces G₁ cell cycle arrest and apoptosis in NIH/3T3 cells. A 5 mM (1 mg/399 µl) solution of KN-93 (Cat. No. 422712) in DMSO is also available.

Cell-permeable, reversible, and competitive inhibitor of rat brain Ca⁺²/calmodulin-dependent protein kinase II (K_i = 370 nM). KN-93 selectively binds to the Calmodulin (CaM) binding site of the enzyme and prevents the association of CaM with CaM Kinase II. Selectively binds to the CaM binding site of the enzyme and prevents the association of CaM with CaMKII. Has no significant effect on protein kinase A activity. Induces G₁ cell cycle arrest and apoptosis in NIH 3T3 cells.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
cam kinase 2

Product competes with ATP.

Reversible: yes

Target K_i: 370 nM against rat brain CaM kinase II

Warning

Toxicity: Irritant (B)

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.

Other Notes

Fan, G.H., et al. 1999. Mol. Pharmacol.56, 39.
Tombes, R.M., et al. 1995. Cell Growth Differ.6, 1063.
Mamiya, N., et al. 1993. Biochem. Biophys. Res. Commun. 195, 608.
Nicki, I., et al. 1993. Biochem. Biophys. Res. Commun.191, 255.
Sumi, M., et al. 1991. Biochem. Biophys. Res. Commun.181, 968.
Tokumitsu, H., et al. 1990. J. Biol. Chem.265, 4315.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable