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KN-62

Cat. No. M1928
KN-62 Structure
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5mg USD 80 In stock
10mg USD 150 In stock
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Biological Activity

KN-62 is a cell-permeable, reversible, and selective inhibitor of CaM kinase II (Ki = 900 nM for rat brain CaM kinase II). KN-62 is also a potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM). KN-62 inhibits the growth of K562 cells in a dose-dependent manner. KN-62 could inhibit the Ca2+/CaM kinase II activity in vivo. However, KN-62 only slightly influenced PC secretion from type II cells stimulated by phorbol 12-myristate 13-acetate, terbutaline and ATP that are known to increase surfactant secretion via the protein kinase C and protein kinase A pathways. KN-62 affects the interaction between calmodulin and Ca2+/CaM kinase II following inhibition of this kinase activity by directly binding to the calmodulin binding site of the enzyme but does not affect the calmodulin-independent activity of already autophosphorylated (activated) enzyme.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 721.84
Formula C38H35N5O6S2
CAS Number 127191-97-3
Purity 99.70%
Solubility DMSO: ≥ 90 mg/mL
Storage at -20°C
References

Inhibition of lung surfactant secretion by KN-62, a specific inhibitor of the calcium- and calmodulin-dependent protein kinase II.
Liu L. Biochem Mol Biol Int. 1998 Jul;45(4):823-30. PMID: 9713707.

KN-62, a specific Ca++/calmodulin-dependent protein kinase inhibitor, reversibly depresses the rate of beating of cultured fetal mouse cardiac myocytes.
Okazaki K, et al. J Pharmacol Exp Ther. 1994 Sep;270(3):1319-24. PMID: 7932185.

KN-62, 1-[N,O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazi ne, a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II.
Tokumitsu H, et al. J Biol Chem. 1990 Mar 15;265(8):4315-20. PMID: 2155222.

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KN 93

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KN-92

KN-92 is an inactive analog of the CaM kinase II inhibitor KN-93.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: KN-62 supplier, CaMK, inhibitors

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