CaMK Inhibitor

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

XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC₅₀ of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects.

(-)-Limonene ((S)-(-)-Limonene) is orally active and can cause mild bronchoconstriction. (-)-Limonene alleviates cytosolic and mitochondrial oxidative stress by inhibiting the increase of calcium ions (Ca²⁺) and Ca²⁺/calmodulin-dependent protein kinase II (CaMKII). It also exerts anti-stress effects by inhibiting the activity of the hypothalamic-pituitary-adrenal (HPA) axis. Additionally, (-)-Limonene can be used as an antibacterial agent in aquaculture.

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.

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

CaMKIIδ-IN-1 (Compound 15e) is a pyrimidine-based inhibitor of CaMKIIδ with an IC₅₀ of 12 nM.

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.

CaMKIIα-IN-1 (Compound 4d) is an orally active Ca²⁺/calmodulin-dependent protein kinase II α (CaMKIIα) inhibitor with a K_D of 219 nM for CaMKIIα WT hub. CaMKIIα-IN-1 has good metabolic stability.

Cucurbitacin IIa (Hemslecin A) is an orally active, blood-brain barrier-permeable EGFR inhibitor with an IC₅₀ of 1.455 nM against human EGFR. Cucurbitacin IIa induces caspase-3-dependent apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton via actin aggregation, arrests the cell cycle at the G2/M phase, and exerts anti-inflammatory activity by inhibiting the EGFR-MAPK signaling pathway. Cucurbitacin IIa can be used in the research of inflammation-related diseases, depression, and cancers such as non-small cell lung cancer.

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.

Lavendustin C is a potent Ca²⁺ calmodulin-dependent kinase II (CaMK II) inhibitor with an IC₅₀ of 0.2 μM. Lavendustin C inhibits EGFR-associated tyrosine kinase (IC₅₀=0.012 μM) and pp60^c-src(+) kinase (IC₅₀=0.5 μM) .

Rimacalib (SMP 114) is a Ca²⁺/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC₅₀s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.

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.

(E)-KN-93 phosphate is a Ca²⁺/calmodulin-dependent protein kinase II (CaMKII) inhibitor with IC₅₀ values of 9 μM and 3 μM against CaMKIIδ_Monomer and CaMKIIδ_Dodecamer, respectively. (E)-KN-93 phosphate can be used in research on epilepsy, depression, and arrhythmias..

CaMKIIδ-IN-1 (Compound 15e) hydrochloride is a pyrimidine-based inhibitor of CaMKIIδ with an IC₅₀ of 12 nM.

Glycyl H-1152 hydrochloride (compound 18) is a glycyl derivative of Rho-kinase inhibitors H-1152 dihydrochloride. Glycyl H-1152 hydrochloride inhibits ROCKII, Aurora A, CAMKII and PKG, with IC₅₀s of 0.0118, 2.35, 2.57 and 3.26 μM respectively. Glycyl H-1152 hydrochloride has higher selective than H-1152 hydrochloride.

Cabamiquine (DDD107498) succinate is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC₅₀ of 1 nM against P. falciparum 3D7. Cabamiquine succinate inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC₅₀ of 2 nM for WT-PfeEF2.

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.