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 제품안내  면역학   Neuroscience  Ion Channel

Calmodulin-Dependent Protein Kinase (CaM Kinase) Inhibitors

Ca2+/Calmodulin-Dependent Protein Kinase인 CaMKK2는 뇌의 시상하부에 존재하며 AMPK의 활성화와 Ca2+의 작용을 중간에서 매개하는 물질입니다.

머크 밀리포아에서는 생체내에서 Ca2+의 binging와 activation 메커니즘 연구에 필요한 inhibitor를 소개합니다.
Merck Millipore
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  • Calmodulin-Dependent Protein Kinase (CaM Kinase) Inhibitors
    • Cat. No. Name Product Biological Activity
    208710 [Ala286]-Ca2+/Calmodulin Kinase II Inhibitor 281-301 CaM Kinase II Inhibitor 281-301, MHRQEAVDCLKKFNARRKLKG-NH2 Acts as a potent inhibitor of CaM kinase II catalytic fragment (IC50 = 2 uM). The inhibition is competitive with respect to ATP and noncompetitive with respect to peptide substrate.
    H-Met-His-Arg-Gln-Glu-Ala-Val-Asp-Cys-Leu-Lys-Lys-Phe-Asn-Ala-Arg-Arg-Lys-Leu-Lys-Gly-NH2
    189480 Autocamtide-2 Related Inhibitory Peptide AIP, (Ala9)-Autocamtide-2, KKALRRQEAVDAL Non-phosphorylatable analog of Autocamtide-2 (Cat. No. 189475) that acts as a highly specific and potent inhibitor of calmodulin-dependent protein kinase II (IC50 = 40 nM). It is about 50 times more potent than [Ala286]-CaM kinase II Inhibitor, 281-301 (Cat. No. 208710).
    H-Lys-Lys-Ala-Leu-Arg-Arg-Gln-Glu-Ala-Val-Asp-Ala-Leu-OH
    189484 Autocamtide-2 Related Inhibitory Peptide II KKKLRRQEAFDAL, A3K/V10F-AIP, AIP-II Acts as a highly specific, potent inhibitor of calmodulin-dependent protein kinase II (CaMKII; IC50 = 4.1 nM). Displays ~10-fold greater potency than AIP. Inhibits PKC at higher concentrations (IC50 = 1 uM) and does not affect the activities of CaMK IV and PKA (IC50 > 100 uM).
    H-Lys-Lys-Lys-Leu-Arg-Arg-Gln-Glu-Ala-Phe-Asp-Ala-Leu-OH
    189485 Autocamtide-2 Related Inhibitory Peptide II, Cell-permeable Ac-RQIKIWFQNRRMKWKKKKKLRRQEAFDAL-OH, Ant-A3K/V10F-AIP, Ant-AIP-II A highly specific, potent, cell-permeable calmodulin-dependent protein kinase II (CaMKII) inhibitor that contains the Antennapedia transport peptide sequence fused to the amino terminus of AIP-II (Cat. No. 189484).
    Ac-Arg-Gln-Ile-Lys-Ile-Trp-Phe-Gln-Asn-Arg-Arg-Met-Lys-Trp-Lys-Lys-Lys-Lys-Lys-Leu-Arg-Arg-Gln-Glu-Ala-Phe-Asp-Ala-Leu-OH
    189482 Autocamtide-2 Related Inhibitory Peptide, Myristoylated Myristoylated AIP, Myr-N-KKALRRQGAVDAL-OH This peptide corresponds to AIP (Cat. No. 189480) which has been myristoylated at the N-terminus, thus enhancing its cell-permeability.
    Myr-N-Lys-Lys-Ala-Leu-Arg-Arg-Gln-Glu-Ala-Val-Asp-Ala-Leu-OH
    208711 Ca2+/Calmodulin Kinase II Inhibitor 281-309 CaM Kinase II Inhibitor 281-309, MHRQETVDCLKKFNARRKLKGAILTTMLA-OH Useful as a calmodulin binding peptide. Inhibits CaM kinase II (IC50 = 80 nM) by blocking Ca2+/calmodulin activation and enzyme active site (IC50 = 2 uM).
    H-Met-His-Arg-Gln-Glu-Thr-Val-Asp-Cys-Leu-Lys-Lys-Phe-Asn-Ala-Arg-Arg-Lys-Leu-Lys-Gly-Ala-Ile-Leu-Thr-Thr-Met-Leu-Ala-OH
    208734 Calmodulin Binding Domain Calmodulin antagonist, CaM kinase II 290-309 Potent calmodulin antagonist. Inhibits activation of calmodulin-dependent protein kinase II (IC50 = 52 nM). Interacts with the catalytic core of CaM kinase II as a pseudosubstrate.
    H-Leu-Lys-Lys-Phe-Asn-Ala-Arg-Arg-Lys-Leu-Lys-Gly-Ala-Ile-Leu-Thr-Thr-Met-Leu-Ala-OH
    208920 Calmodulin Kinase IINtide KRPPKLGQIGRAKRVVIEDDRIDDVLK-OH A potent and specific inhibitor of CaMK II. Does not affect the activities of CaMK I, CaMK IV, CaMKK, PKA, or PKC. The peptide sequence corresponds to the inhibitory domain of CaMK IIN.
    H-Lys-Arg-Pro-Pro-Lys-Leu-Gly-Gln-Ile-Gly-Arg-Ala-Lys-Arg-Val-Val-Ile-Glu-Asp-Asp-Arg-Ile-Asp-Asp-Val-Leu-Lys-OH
    208921 Calmodulin Kinase IINtide, Myristoylated Myr-N-GGGKRPPKLGQIGRAKRVVIEDDRIDDVLK-OH The myristoylated form of CaMK IINtide (Cat. No. 208920). The peptide has been modified at the amino terminal lysine with the addition of three glycine residues and myristoylated to improve cell-permeability.
    Myr-N-Gly-Gly-Gly-Lys-Arg-Pro-Pro-Lys-Leu-Gly-Gln-Ile-Gly-Arg-Ala-Lys-Arg-Val-Val-Ile-Glu-Asp-Asp-Arg-Ile-Asp-Asp-Val-Leu-Lys-OH
    208922 CaMKII Inhibitor, CK59 2-(2-Hydroxyethylamino)-6-aminohexylcarbamic acid tert-butyl ester-9-isopropylpurine, CK59 A cell-permeable Olomoucine (Cat. Nos. 495620 & 495624) analog that acts as a CaMKII inhibitor (IC50 <10 uM) and inhibits insulin-stimulated glucose uptake (IC50 ≤5 uM) and GLUT4 membrane translocation (IC50 = 100 uM) in 3T3-L1 adipocytes.
    371963 H-89, Dihydrochloride N-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl A cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase A (Ki = 48 nM). Inhibits other kinases only at much higher concentrations: CaM kinase II (Ki = 29.7 uM), casein kinase I (Ki = 38.3 uM), myosin light chain kinase (Ki = 28.3 uM), protein kinase C (Ki = 31.7 uM), and ROCK-II (IC50 = 270 nM).
    371964 HA 1004, Dihydrochloride N-(2-Guanidinoethyl)-5-isoquinolinesulfonamide, 2HCl A cell-permeable, reversible, and ATP-competetive inhibitor of protein kinase A (Ki = 2.3 uM), CaM kinase II (Ki = 13 uM), myosin light chain kinase (Ki = 150 uM), protein kinase C (Ki = 40 uM), and protein kinase G (Ki = 1.3 uM). An intracellular Ca2+ antagonist with no effect on cardiac function.
    420297 InSolution™ K-252a, Nocardiopsis sp. - Formulation : A 1 mM (100 ug/214 ul) solution of K-252a (Cat. No. 420298) in DMSO.
    420298 K-252a, Nocardiopsis sp. - A cell-permeable, reversible, and ATP-competitive inhibitor against multiple protein kinases, including, but not limited to, CaM kinase II, myosin light chain kinase, protein kinase A, protein kinase C, protein kinase G, NGF receptor gp140trk, its transforming trk oncogenes, and the related neurotrophin receptors gp145trkB and gp145trkC. Reported to induce apoptosis and cell cycle arrest by decreasing Cdk1 and Cdc25c activity in T98G cells and inhibit Flt3 phosphorylation in Flt3/Itd-BaF3 cells.
    422706 KN-62 1-[N,O-bis-(5-Isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine A cell-permeable, reversible, and selective inhibitor of CaM kinase II (Ki = 900 nM for rat brain CaM kinase II) that binds directly to the calmodulin binding site of the enzyme.
    422709 KN-92 2-[N-(4-Methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine, Phosphate Useful as a negative control for KN-93 (Cat. No. 422708), a Ca2+/CaM kinase II inhibitor.
    422708 KN-93 2-[N-(2-hydroxyethyl)]-N-(4-methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine) A cell-permeable, reversible and competitive inhibitor of rat brain CaM kinase II (Ki = 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.
    422712 InSolution™ KN-93 - Formulation : A 5 mM (1 mg/399 ul) solution of KN-93 (Cat. No. 422708) in DMSO.
    422711 KN-93, Water-Soluble - A water-soluble form of the CaM kinase II inhibitor KN-93 (Cat. No. 422708).
    234450 Lavendustin C Compound 5, 5-(N-2′,5′-Dihydroxybenzyl)aminosalicylic Acid A cell-permeable, reversible, substrate competitive, and potent inhibitor of pp60c-src (IC50 = 200 nM) and CaM kinase II (IC50 = 200 nM).
    529581 PP1 Analog II, 1NM-PP1 Mutant Kinases Inhibitor II, 4-Amino-1-tert-butyl-3-(1′-naphthylmethyl)pyrazolo[3,4-d]pyrimidine, NM A cell-permeable and reversible PP1 analog (Cat. No. 529579) that acts as a potent and selective ATP-competitive inhibitor of mutant kinases over wild-type (IC50 = 3.2 nM for T339G, c-Fyn-as1 vs. 1.0 uM for c-Fyn; 4.3 nM for I338G, v-src-as1 vs. 28 uM for v-src; 5 nM for F80G, CDK2-as1 vs. 29 uM for CDK2; 8 nM for F89G, CAMK IIα-as1 vs. 24 uM for CAMKII; 120 nM for T315A, c-Abl-as2 vs. 3.4 uM for c-Abl).
    570250 STO-609 7H-Benz[de]benzimidazo[2,1-a]isoquinoline-7-one-3-carboxylic Acid, Acetate, 7-Oxo-7H-benzimidazo[2,1-a]benz[de]isoquinoline-3-carboxylic Acid, Acetate A cell-permeable and reversible naphthoyl fused benzimidazole compound that acts as a highly selective, potent, ATP-competitive inhibitor of Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK) [IC50 = 120 ng/ml and 40 ng/ml for CaM-KKα and CaM-KKβ isoforms, respectively]. Binds to the catalytic domain of CaM-KK, and inhibits autophosphorylation. Does not significantly affect the activities of CaM-KII, MLCK (IC50 = ~10 ug/ml), CaM-KI, CaM-KIV, PKA, PKC, and p42 MAP kinase (IC50 >10 ug/ml). Has also been reported to inhibit phosphorylation of AMP-activated protein kinase (AMPK).