CaMK Inhibitor

STO-609 is a selective and cell-permeable inhibitor of the Ca²⁺/calmodulin-dependent protein kinase kinase (CaM-KK), with K_i values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC₅₀ ~0.02 g/ml.

SKF-96365 hydrochloride is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 hydrochloride reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 hydrochloride inhibits voltage-gated sodium current (cardiac I_Na/NaV1.5) and slows myocardial conduction. SKF-96365 hydrochloride inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 hydrochloride induces G₂/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 hydrochloride alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 hydrochloride reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 hydrochloride inhibits the growth of colorectal cancer xenografts in nude mice. SKF-96365 hydrochloride is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia.

A-484954 is a highly selective eukaryotic elongationfactor-2 kinase(eEF2K) inhibitor, with an IC₅₀ of 280 nM.

Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.

ANDS (1-Amino-8-naphthol-2,4-disulfonic acid) is an orally active inhibitor of CaMKP (IC₅₀ = 6.4 μM; K_i = 3.6 μM) and CaMKP‑N (IC₅₀ = 6.6 μM). ANDS binds unacetylated p53 and restores p53 activity by disrupting ANP32B-p53 interaction. ANDS inhibits chronic myeloid leukemia (CML) cell proliferation, impairs leukemic stem cells (LSC) function and prolongs survival in CML mouse model while sparing normal progenitor cells. ANDS can be used to study the eradication of LSCs and the overcoming of tyrosine kinase inhibitor (TKI) resistance in CML. ANDS can be used to study breast cancer.

Trifluoperazine, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine is a potent α1-adrenergic receptor antagonist. Trifluoperazine is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine can be used for the research of schizophrenia. Trifluoperazine acts as a reversible inhibitor of influenza virus morphogenesis.

Neoandrographolide is a diterpenoid compound isolated from Andrographis paniculata. Neoandrographolide inhibits osteoclasts differentiation and bone resorption through inhibition of MAPK/NF-κB/PI3K/AKT/GSK3β/PPAR/CAMK signaling pathway. Neoandrographolide inhibits apoptosis in rat embryonic ventricular cardiomyocytes. Neoandrographolide inhibits iNOS and the generation of ROS, activates eNOS, exhibiting anti-inflammatory and hypolipidemic activity.

CS640 (Compound 19) is a chemical probe and a calmodulin-dependent kinase inhibitor. CS640 inhibits CaMK1D, CaMK1B, CaMK1A, CaMK1G, MEK5, RIPK4, mLK3 and PIP5K1, with IC₅₀ values of 8, 3, 1, 1, 25 nM, 5.69, 2.75 and 11.2 μM, respectively. CS640 blocks Aβ-induced hyperphosphorylation of tau protein at the Thr181 site, but fails to protect primary mouse cortical neurons from Aβ-induced toxic damage. CS640 is applicable to research related to Alzheimer's disease.

CS587 is a specific inhibitor of CaMK1D with neurocytotoxicity at 10 μM. CS587 modulates the sensitivity of neuronal cells to Aβ oligomer toxicity.

Alisol B is a triterpene with diverse biological activities. Alisol B binds human soluble epoxide hydrolase (sEH) with a K_i of 5.97 μM and reduces sEH activity. Alisol B inhibits RANKL-induced JNK phosphorylation, NFATc1 and c-Fos expression, osteoclast formation, mature osteoclast pit-forming and actin ring activity, and SERCA pump activity. Alisol B induces calcium mobilization, CaMKK-AMPK-mTOR pathway activation, autophagic flux, autophagosome formation, G₁ phase cell cycle arrest, endoplasmic reticulum stress, unfolded protein responses, and cancer cell apoptosis. Alisol B can be used for the research of hypercalcemia, osteoporosis, rheumatoid arthritis, periodontitis, acute kidney injury, and breast cancer.

Sordarin sodium is an eEF2 inhibitor and antibiotic. Sordarin sodium's function is dependent on the diphthamide modification on eEF2. Sordarin sodium inhibits protein synthesis by preventing the binding of eEF2 to the ribosome complex. Sordarin sodium has antifungal activity.

CAMK1D-IN-1 (compound I) is an inhibitor of CAMK1D, targeting cytotoxic T lymphocyte (CTL)-resistant tumor cells. CAMK1D impairs CTL-induced death receptor signaling and apoptosis by inhibiting caspases, making it a key and effective target for PD-L1-refractory tumors.

TIM-063 is a selective and cell-permeable CaMKK inhibitor, ATP competitive inhibitor, can directly target the catalytic domain of CaMKK, with the K_i values of 0.35 μM and 0.2 μM for CaMKKα and CaMKKβ, respectively, the IC₅₀ values are 0.63 μM and 0.96 μM, respectively.

SKF-96365 is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 inhibits voltage-gated sodium current (cardiac I_Na/NaV1.5) and slows myocardial conduction. SKF-96365 inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 induces G₂/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 inhibits the growth of colorectal cancer xenografts in nude mice. SKF-96365 is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia.

Purine riboside-5'-O-triphosphate, an active metabolite of Nebularine (HY-103694), acts as an inhibitor of DNA primase ATP and GTP polymerization activities, with IC₅₀ values of 35 µM and 28 µM for the human enzyme, respectively. Purine riboside-5'-O-triphosphate also inhibits calmodulin-dependent protein kinase II (CaMKII) with a K_i value of 590 µM.

Trifluoperazine (dihydrochloride) (Standard) is the analytical standard of Trifluoperazine (dihydrochloride). This product is intended for research and analytical applications. Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.

STO-609 acetate is a selective and cell-permeable inhibitor of the Ca²⁺/calmodulin-dependent protein kinase kinase (CaM-KK), with K_i values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 acetate inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC₅₀ ~0.02 g/ml.

Trifluoperazine dimaleate, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dimaleate is a potent α1-adrenergic receptor antagonist. Trifluoperazine dimaleate is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dimaleate is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dimaleate can be used for the research of schizophrenia. Trifluoperazine dimaleate acts as a reversible inhibitor of influenza virus morphogenesis.

Prenylamine (lactate) (Standard) is the analytical standard of Prenylamine (lactate). This product is intended for research and analytical applications. Prenylamine lactate is a calcium-modulating protein (CaM) antagonist that inhibits CaM-dependent enzymes and can slowly relax smooth muscle preparations. The effect of Prenylamine lactate on smooth muscle is not inhibited by the calcium agonist Bay K 8644 (HY-10588). Reports suggest that under low heart rate conditions, Prenylamine seems to enhance voltage-dependent transmembrane calcium currents.

Trifluoperazine-d₃ (dihydrochloride) is deuterium labeled Trifluoperazine (dihydrochloride). Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.