Merck UK - Calbiochem - Inhibitors: Phosphorylation/Dephosphorylation

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		Technical Information

		Calbiochem Information

		Inhibitor Resource

		Phosphorylation Dephosphorylation

		AKT
		AMPK
		Aurora Kinase
		Cam Kinase
		Casein Kinase
		Checkpoint Kinase
		Cyclin-dependent Kinase
		DNA-Dependent Protein Kinase
		Glycogen Synthase Kinase
		c-Jun N-Terminal Kinase
		IP3 Kinase & TGF-b Receptor I Kinase
		MAP Kinase
		MLCK
		PI 3 Kinase
		Protein Kinase A
		Protein Kinase C
		Protein Kinase G
		Protein Phosphatase
		Protein Tyrosine Kinase
		Raf Kinase
		Rho Kinase
		Sphingosine Kinase

Phosphorylation/Dephosphorylation: CaM Kinase Inhibitors

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Table 1: Selected CAMK Inhibitors | Products

Many effects of Ca^²⁺ are mediated by Ca^²⁺/calmodulin (CaM)-dependent protein kinases (CaM kinases). CaM Kinases constitute a family of structurally related enzymes that include phosphorylase kinase, myosin light chain kinase, and CaM kinases I-IV. CaM Kinase II, one of the best-studied multifunctional enzymes, is found in high concentrations in neuronal synapses, and in some regions of the brain it may constitute up to 2% of the total protein content. Activation of CaM kinase II has been linked to memory and learning processes in the vertebrate nervous system. CaM Kinase II is a complex of about 12 subunits that exist in four differentially expressed forms (a, b, g, and d). In the inactive state there is a strong interaction between the inhibitory and catalytic domains of the enzyme. The binding of Ca^²⁺/CaM allows the catalytic domain to phosphorylate the inhibitory domain. Once activated, CaM Kinase II retains significant activity even after the withdrawal of Ca²⁺, thereby prolonging the duration of kinase activity. Several synthetic and naturally occurring compounds have been shown to bind CaM in a Ca²⁺-dependent manner and block the activation of CaM-dependent enzymes. These compounds have been extensively used in investigating the mechanism of Ca²⁺-binding and activation in biological systems.

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Table 1: CAMK Inhibitors

Product	Cat. No.	MW	Comments
Autocamtide-2 Related Inhibitory Peptide	189480	1497.8	A highly specific and potent inhibitor of Ca²⁺/CaM-dependent protein kinase II (IC₅₀ = 40 nM).
Autocamtide-2 Related Inhibitory Peptide, Myristoylated	189482	1708.1	A cell-permeable analog of AIP (Cat. No. 189480).
Autocamtide-2 Related Inhibitory Peptide II	189484	1602.9	A highly specific, potent inhibitor of calmodulin-dependent protein kinase II (CaMKII) with an IC₅₀ of 4.1 nM. Displays ~ 10-fold greater potency than AIP (Cat. No. 189480).
Autocamtide-2 Related Inhibitory Peptide II, Cell-Permeable	189485	3873.7	A cell-permeable derivative of Autocamtide-2 Related Inhibitory Peptide II (Cat. No. 189484).
Ca²⁺/Calmodulin Kinase II (281 - 309) Inhibitor	208711	3374.1	Potent inhibitor of Ca²⁺/CaM-dependent protein kinase II (IC₅₀ = 80 nM).
[Ala²⁸⁶]-Ca²⁺/Calmodulin Kinase II Inhibitor (281 - 301)	208710	2528.1	Inhibits CaM kinase II (IC₅₀ = 2 mM).
Calmodulin Binding Domain	208734	2274.3	Inhibits Ca²⁺/CaM-dependent protein kinase II (IC₅₀ = 52 nM).
Calmodulin Kinase IINtide	208920	3115.7	A potent and specific inhibitor of CaMK II (IC₅₀ = 50 nM for both the total and Ca²⁺-independent activities of CaMK II). Does not affect the activities of CaMK I, CaMK IV, CaMKK, PKA, or PKC.
Calmodulin Kinase IINtide, Myristoylated	208921	4698.3	A myristoylated derivative of Calmodulin Kinase IINtide (Cat. No. 208920).
K-252a, Nocardiopsis sp.	420298	467.5	A highly potent inhibitor of Ca²⁺/CaM kinase (K_i = 1.8 nM). Also inhibits myosin light chain kinase (K_i = 17 nM), protein kinase A (K_i = 25 nM), and protein kinase C (K_i = 25 nM). See also Cat. No. 420297.
KN-62	422706	721.9	Selectively inhibits rat brain Ca²⁺/CaM-dependent protein kinase II (K_i = 900 nM) by binding directly to the calmodulin binding site of the enzyme.
KN-92	422709	555.0	A negative control compound for KN-93.
KN-93	422708	501.0	Inhibitor of rat brain Ca²⁺/CaM-dependent protein kinase II (K_i = 370 nM). See also Cat. No. 422712.
KN-93, Water-Soluble	422711	599.0	Inhibitor of rat brain Ca²⁺/CaM-dependent protein kinase II (K_i = 370 nM).
Lavendustin C	234450	275.3	Inhibitor of Ca²⁺/CaM kinase II (IC₅₀ = 200 nM) and p60^c-src (IC₅₀ = 200 nM).
Staurosporine, Streptomyces sp.	569397	466.5	A pan-kinase inhibitor; IC₅₀ = 20 nM for CaM kinase.
STO-609	570250	374.4	A cell-permeable, ATP-competitive inhibitor of CaM kinase kinase (CaM-KK) (IC₅₀ = 320 nM and 106 nM for CaM-KKa and CaM-KKb isoforms, respectively).

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Inhibitors: Calmodulin-Dependent Protein Kinase (CaM Kinase)

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