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Neuroscience

Melanocortin Receptor

Neuropeptide Y Receptor

Serotonin Transporter

(51)

iGluR

(130)

CaMK

CAMK, also written as CaMK, is an abbreviation for the Ca2+/calmodulin-dependent protein kinase class of enzymes. CAMKs are activated by increases in the concentration of intracellular calcium ions (Ca2+) and calmodulin. When activated, the enzymes transfer phosphates from ATP to defined serine or threonine residues in other proteins, so they are serine/threonine-specific protein kinases. Activated CAMK is involved in the phosphorylation of transcription factors and therefore, in the regulation of expression of responding genes. CAMK also works to regulate the cell life cycle (i.e. programmed cell death), rearrangement of the cell's cytoskeletal network, and mechanisms involved in the learning and memory of an organism.There are 2 common types of CAM Kinase proteins: specialized and multi-functional CAM kinases.

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Calmodulin-Dependent Protein Kinase II 290-309 acetate

TP1271L

Calmodulin-Dependent Protein Kinase II 290-309 acetate is an effective antagonist of Ca2+ calmodulin-dependent protein kinase II (IC50 = 52 nM).

$133

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Trifluoperazine

T8389117-89-5

Trifluoperazine (trifluoroperazine) is a Dopamine D2 receptor inhibitor(IC50 : 1.2 nM), and Treatment of schizophrenia.

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CaMKP Inhibitor

T215952789-62-5

CaMKP Inhibitor can inhibit CaMKP.

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KN-93

T2697139298-40-1

KN-93 is a selective inhibitor of Ca2+ calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase.

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KN-93 Phosphate

T26061913269-12-1

KN-93 (Phosphate) can competitively block the binding of calmodulin to the corresponding kinase. It is a calcium calmodulin-dependent kinase II (CaMKII) inhibitor with a Ki of 370 nM. It can also inhibit the proliferation of human hepatic stellate cells.

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Melatonin

T165973-31-4

Melatonin (Melatonine) is a natural hormone secreted by the pineal gland that activates melatonin receptors. Melatonin is a hormone that regulates the biological clock and also has antioxidant and anti-inflammatory activities.

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Nifedipine

T114621829-25-4

Nifedipine (Procardia) is a dihydropyridine calcium channel blocking agent. Nifedipine inhibits the transmembrane influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, causing dilatation of the main coronary and systemic arteries and decreasing myocardial contractility. This agent also inhibits the drug efflux pump P-glycoprotein which is overexpressed in some multi-drug resistant tumors and may improve the efficacy of some antineoplastic agents.

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Calmidazolium chloride

T1066757265-65-3

Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist with a Kd of 3 nM, which inhibits CaM-dependent phosphodiesterase (IC50 = 0.15 μM) and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase (IC50 = 0.35 μM). It also induces apoptosis in certain cancer cell lines.

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Tanshinone IIA sulfonate sodium

T294669659-80-9

Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.

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STO-609

T354652029-86-4

STO-609 is a specific and cell-permeable inhibitor of the Ca2+ calmodulin-dependent protein kinase kinase (CaM-KK) for recombinant CaM-KKα KKβ (Ki: 80 15 ng mL).

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Psoralenoside

TN1008905954-17-8

Psoralenoside is a natural product isolated from the fruits of Psoralea corylifolia, shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.

$122

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Rottlerin

T1679182-08-6

Rottlerin (NSC-56346) is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation.

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CALP2 acetate(261969-04-4 free base)

TP1909L1

CALP2 acetate is an antagonist of calmodulin showing high affinity for binding to the CaM EF-hand Ca2+-binding site with a Kd of 7.9 µM. CALP2 acetate potently inhibits of adhesion and degranulation. CALP2 acetate is also a strong activator of alveolar macrophages. CALP2 acetate inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca2+ concentrations.

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lavendustin C

T4185125697-93-0

lavendustin C (NSC 666251) is a potent inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase.

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NH125

T6605278603-08-0

NH125 is a selective eEF-2 kinase inhibitor with IC50 of 60 nM, >125-fold selectivity over PKC, PKA, and CaMKII, and also a potent histidine kinase inhibitor.

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KN-62

T2694127191-97-3

KN-62 is a potent and specific Ca2+ calmodulin-dependent protein kinase II (CaMKII) inhibitor with Ki of 0.9 μM.

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CALP1 acetate

TP1910L1

CALP1 acetate is a calmodulin (CaM) agonist (Kd of 88 µM) that binds to the CaM EF-hand Ca2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) by inhibiting the open of calcium channel. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity.

$133

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Berbamine

T3S0807478-61-5

Berbamine is a natural product extracted from Phellodendron amurense. It acts as a calcium channel blocker and possesses anti-tumor, immunomodulatory, and cardiovascular effects.

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Phenoxybenzamine hydrochloride

T115863-92-3

Phenoxybenzamine hydrochloride (NCI-c01661) is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen.

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Perphenazine

T109058-39-9

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

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A-484954

TQ0137142557-61-7

A-484954 (A 484954) is a highly specific eukaryotic elongation factor-2 (eEF2, IC50: 280 nM) inhibitor.

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W-7 hydrochloride

T2079261714-27-0

W-7 hydrochloride (W-7 HCl), a calmodulin antagonist, inhibits Ca2+-calmodulin-dependent myosin light chain kinase and phosphodiesterase, W-7 hydrochloride induces apoptosis and has antitumor activity.

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Y-33075 dihydrochloride

T13384L173897-44-4

Y-33075 dihydrochloride is a selective inhibitor of ROCK with an IC50 of 3.6 nM.

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CaMKII-IN-1

T148601208123-85-6

CaMKII-IN-1, a potent and highly selective inhibitor of CaMKII (IC50 = 63 nM), exhibits over 100-fold higher selectivity for CaMKII compared to CaMKIV, MLCK, p38a, Akt1, and PKC.

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Dibucaine

T036485-79-0

Dibucaine (Cinchocaine), a local anesthetic of the amide type, is now usually used for surface anesthesia.

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KN-92 hydrochloride

T85431431698-47-3

KN-92 hydrochloride is an inactive derivative of the selective Ca2+ calmodulin-dependent kinase II (CaMKII) inhibitor KN-93, which competitively blocks CaM binding to the kinase with a Ki of 370 nM.

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Praeruptorin A

T377773069-27-9

Praeruptorin A ((+)-Praeruptorin A) has the potential to inhibit migration fusion of preosteoclasts in vitro and bone erosion in vivo by targeting calmodulin and inhibiting the Ca(2+) calmodulin-CaMKIV-CREB-NFATc1 and or Ca(2+) calmodulin-calcineurin-NFATc1 signaling axis.

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Promethazine

T044560-87-7

Promethazine (Proazamine) is an analogue of anti-glaucoma prostaglandin (PG) .

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W-9 hydrochloride

T2352569762-85-2

W-9 hydrochloride is a calmodulin antagonist.

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Trifluoperazine dihydrochloride

T1222440-17-5

Trifluoperazine dihydrochloride (SKF5019) is a potent dopamine D2 receptor inhibitor used as an antipsychotic and an antiemetic.

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A-7 hydrochloride

T2253879127-24-5

A-7 hydrochloride is a calmodulin antagonist and causes alterations in the subpopulation of CD44+CD24- in MDA-MB-231 cells.

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STO-609 acetate

T36501173022-21-3

STO-609 acetate is selective, cell-permeable inhibitor of Ca2+-calmodulin-dependent protein kinase kinase (Ki: 80 15 ng ml, for CaM-KKα KKβ); competes for the ATP-binding site. It displays > 80-fold selectivity over CaMK1 2 4, PKC, MLCK, PKA and p42 MAPK.

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A-3 hydrochloride

T1406978957-85-4

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It inhibits PKC and casein kinase I with Ki values of 47 μM and 80 μM, respectively[1], and also inhibits PKA (Ki=4.3 μM), casein kinase II (Ki=5.1 μM), and myosin light chain kinase (MLCK) (Ki=7.4 μM).

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W-13 hydrochloride

T2352288519-57-7

W-13 hydrochloride (W-13 HCl) is a calmodulin antagonist.

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Cloxacepride

T6804865569-29-1In house

cloxacepride is a CaM antagonist that is used to treat asthma disease.

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Elziverine

T6806495520-81-3In house

Elziverine is an orally available small molecule calmodulin antagonist.Elziverine in vitro treatment inhibited Ca-loading-induced acanthocyte formation in SHRSP, WKY, and Wistar rats in a concentration-dependent manner.Elziverine can be used for the treatment of neurological disorders, and may be used for the study of cognitive disorders.

$168

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Syntide 2 acetate(108334-68-5 free base)

TP1403L

Syntide-2 acetate is a synthetic peptide recognized as a substrate by Ca2+ calmodulin-dependent protein kinase II (CaMKII; Km = 12 μM).

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Autocamtide 2 TFA(129198-88-5 free base)

TP1217L

Autocamtide 2 TFA is a highly selective peptide substrate of calcium calmodulin-dependent protein kinase II (CaMKII). Autocamtide 2 TFA can be used in the CaMKII activity assay.

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W-5 hydrochloride

T2352361714-25-8

W-5 hydrochloride (N-(6-Aminohexyl)-1-naphthalenesulfonamide HCl) is a potent calmodulin antagonist.

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Autocamtide-2-related inhibitory peptide, myristoylated acetate(201422-04-0 free base)

TP1921L1

Autocamtide-2-related inhibitory peptide, myristoylated acetate is a CaM kinase II inhibitor; enhanced cell permeable derivative of Autocamtide-2-related inhibitory peptide.

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Autocamtide-2-related inhibitory peptide

TP2310167114-91-2

Autocamtide-2-related inhibitory peptide is a potent and highly specific inhibitor of CaMKII, with an IC50 of 40 nM.

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KN-92 phosphate

T45301135280-28-2

KN-92 phosphate (KN92-H3PO4) is an inactive derivative of KN-93. KN-93 is a selective inhibitor of Ca2+ calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).

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CaM kinase II inhibitor TFA salt

TP1216

CaM kinase II inhibitor TFA salt (Autocamtide-2-related inhibitory peptide (TFA)) is a highly specific and potent inhibitor of CaMKII with an IC50 of 40 nM.

$106

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AC3-I, myristoylated

T80269

Myristoylated AC3-I is a biologically active peptide and a myristoylated variant of the Autocamtide-3-Derived Inhibitory Peptide (AC3-I). It acts as a highly specific inhibitor of Calmodulin-Dependent Protein Kinase II (CaMKII) with enhanced resistance to proteolysis. This compound is a derivative of Autocamtide-3, where the Thr-9 phosphorylation site is replaced by Ala.

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CaMKIIα-PHOTAC

T79718

CaMKIIα-PHOTAC is a photochemically targeted chimera (PHOTAC) that specifically targets Ca2+ calmodulin-dependent protein kinase II α (CaMKIIα), facilitating its ubiquitination and subsequent proteasome-mediated degradation when exposed to specific light wavelengths. Under illumination, CaMKIIα-PHOTAC diminishes synaptic functions and weakens evoked field excitatory postsynaptic potentials in the mouse hippocampus, impacting physiological responses and sustaining long-term potentiation and memory functions within dendritic domains [1].

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Calmodulin Kinase IINtide, Myristoylated

T80549

Myristoylated Calmodulin Kinase IINtide (Myr-CaMKIINtide) serves as a selective and noncompetitive inhibitor of CaMKII [1].

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TAT-CN21

TP2862

TatCN21, with an IC 50 of 77 nM, serves as a potent and selective inhibitor peptide of the calcium calmodulin-dependent protein kinase II (CaMKII), a ubiquitously-expressed multifunctional serine threonine protein kinase. It is particularly useful in research pertaining to ischemia and neurodegenerative diseases.

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FO-4-15

T2002031030759-58-0

FO-4-15 is an activator of mGluR1 CaMKIIα. It exhibits protective effects against H2O2 in human neuroblastoma (SH-SY5Y) cells. In mice with Alzheimer's disease, FO-4-15 enhances cognitive function by activating the mGluR1 CaMKIIα pathway, reducing Aβ accumulation, Tau hyperphosphorylation, and synaptic damage.

$1,520

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