PKA Inhibitor

PKItide exhibits an IC₅₀ of 0.2 μM for cAMP-PK.

Sitagliptin-d₄ (MK-0431-d₄) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.

Phoenixin-14 (PNX-14) TFA is an endogenous neuropeptide with multiple biological activities, and serves as the endogenous ligand of GPR173. Phoenixin-14 TFA reduces ROS production by inhibiting the HMGB1/TLR4/MyD88/NF-κB signaling axis, thereby exerting antioxidant and mitochondrial protective effects. Phoenixin-14 TFA inhibits FOXO3 phosphorylation by upregulating SIRT3 expression, suppresses apoptosis, and improves myocardial systolic/diastolic function. Phoenixin-14 TFA resists ferroptosis by activating the ATF4/SLC7A11/GPX4 axis; it activates ERK1/2 phosphorylation via GPR173. Phoenixin-14 TFA can be used in researches on neuroprotection, diabetes, cardiomyopathy, reproductive protection and so on.

TX-1918 is an inhibitor for eukaryotic elongation factor 2 kinase (eEF2-K) and Src kinase with IC₅₀ of 0.44 and 4.4 μM, respectively. TX-1918 exhibits cytotoxicity in cell HepG2 and HCT116, with IC₅₀ of 2.07 and 230 μM, respectively. TX-1918 inhibits the C-terminal domain of HIV-1 CA (CA CTD)(IC₅₀ =3.81 μM), and inhibits the viral replication (IC₅₀ =15.16 μM).

HA-100 hydrochloride is a potent protein kinase inhibitor, with IC₅₀s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 hydrochloride also used as a ROCK inhibitor.

PKA-IN-2 (Compound j1) is a serine/threonine kinase J-PKAcα-targeting inhibitor with an IC₅₀ of 6.3 nM. PKA-IN-2 can be used for liver cancer like fibrolamellar hepatocellular carcinoma research.

GSK-3α/β-IN-1 is GSK-3α/β inhibitor with IC₅₀ s of 0.265 μM and 0.255 μM for GSK-3α and GSK-3β, respectively. GSK-3α/β-IN-1 also inhibits PKA with an IC₅₀ of 0.188 μM. GSK-3α/β-IN-1 potently inhibits cell viability of three Glioblastoma (GBM) cell lines (IC₅₀ : 3-6 μM, 72 h) with no toxicity to human astrocytes and good metabolic stability. GSK-3α/β-IN-1 has potential CNS activity in all-human blood-brain barrier (BBB) model of GBM.

Rp-8-Br-cAMPS is an analog of cAMP and an inhibitor of PKA. Rp-8-Br-cAMPS occupies cAMP binding sites on PKA type I regulatory subunits, thereby preventing PKA dissociation and activation. Rp-8-Br-cAMPS can be used in the study of tumors and retrovirus-induced immune deficiency. Rp-8-Br-cAMPS also inhibits insulin secretion.

HA-100 dihydrochloride is a potent protein kinase inhibitor, with IC₅₀s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 dihydrochloride also used as a ROCK inhibitor.

Antifungal agent-169 (compound 5p) is an antifungal agent that inhibits fluconazole (HY-B0101)-susceptible Candida albicans SC5314 with an MIC₅₀ of 0.28 μM. Antifungal agent-169 reduces the expression levels of cAMP-PKA pathway-related genes including RAS1, EFG1, BCR1, ECE1 and HWP1 in Candida albicans. Antifungal agent-169 inhibits biofilm formation and hyphal growth of Candida albicans. Antifungal agent-169 can be used in studies related to Candida albicans infection.

GEM-231 sodium scrambled negative control is the sequence scrambled negative control of GEM-231 sodium.

PKI (5-22) is a specific inhibitory peptide targeting the catalytic subunit of protein kinase A (PKA) and contains the active region of PKI. PKI (5-22) inhibits the enzymatic activity of the PKA catalytic subunit-like protein in Trypanosoma equiperdum. PKI (5-22) can be used in the research of trypanosomiasis.

GSK466317A is a PKA inhibitor, with an IC₅₀ of 12.59 μM. GSK466317A also inhibits GRK1, GRK2, and GRK5, with IC₅₀s of 1000, 31.62, and 39.81 μM, respectively.

Protein kinase inhibitor 7 is an inhibitor for protein kinase A and protein kinase C. Protein kinase inhibitor 7 affects autocrine motility factor (AMF) signaling pathway, without affecting the cell motility.

Tetramisole is an orally active, selective inward rectifier potassium channel agonist with an EC₅₀ of approximately 30 μM for the Kir2.1 subunit. Tetramisole is also an anti-nematode agent that blocks neuromuscular transmission by non-competitive depolarization. Tetramisole promotes the forward transport of Kir2.1 channels, hyperpolarizes the resting potential (RP), shortens the action potential duration (APD), inhibits intracellular calcium overload and the PKA signaling pathway, and exerts anti-arrhythmic and anti-myocardial remodeling activities. Tetramisole can be used in cardiac electrophysiology research and research related to myocardial ischemia and heart failure.

Kemptide, 5-FAM labeled is a 5-FAM labeled Kemptide (HY-P0248). Kemptide is a phosphate acceptor peptide that serves as a synthetic substrate for PKA (Km = 16 μM). The corresponding fluorescent and biotinylated peptides are also proven to be good substrates for PKA.

ME-3407 (EF-4040) is a H⁺-K⁺-ATPase redistribution disruptor and myosin light chain kinase (MLCK) and protein kinase A inhibitor. ME-3407 blocks gastric acid secretion and aminopyrine accumulation by inhibiting microsomal-to-apical membrane redistribution of H⁺-K⁺-ATPase and suppressing MLCK-mediated myosin light chain phosphorylation. ME-3407 is promising for research of peptic ulcer.

Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC₅₀s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.

Sitagliptin (MK-0431) hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin hydrochloride blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin hydrochloride can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes.

RI-STAD-2 is a high-affinity interfering peptide that regulates the subunit RI of protein kinase A (PKA). RI-STAD-2 interferes with the binding of AKAPs and PKA-RI by simulating the interaction between AKAPs' α-helix domain and PKA-RI's dimerization/anchoration (D/D) domain, thereby affecting PKA activity and intracellular localization. RI-STAD-2 can be used to study the role of AKAPs interaction with PKA-RI in pathological processes such as cardiovascular disease and cancer.