PKA Inhibitor

Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC₅₀s=4-9 nM) and ζ (IC₅₀=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides.

LX7101 monohydrochloride is a potent LIM-kinase, ROCK and PKA inhibitor with IC₅₀s of 24 nM, 1.6 nM, 10 nM and <1 nM for LIMK1, LIMK2, ROCK2 and PKA, respectively. LX7101 monohydrochloride proves significantly selective for LIMK2 with IC₅₀ values of 4.3 nM and 32 nM for LIMK2 and LIMK1 at 2 μM ATP, respectively. LX7101 monohydrochloride has the potential for ocular hypertension and associated glaucoma research.

Sitagliptin (Standard) is the analytical standard of Sitagliptin (HY-13749). This product is intended for research and analytical applications. 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.

H-89 (Standard) is the analytical standard of H-89 (HY-15979). This product is intended for research and analytical applications. H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein K_inase (protein K_inase A) with IC₅₀ of 48 nM and has weak inhibition on PKG, PKC, Casein K_inase, and others K_inases.

Sitagliptin-d₆ (MK-0431-d₆) 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.

4-Ethylresorcinol (Standard) is the analytical standard of 4-Ethylresorcinol (HY-W015782). This product is intended for research and analytical applications. 4-Ethylresorcinol is a derivative of resorcinol and can serve as a substrate for tyrosinase. 4-Ethylresorcinol has anti-hyperpigmentation and antioxidant effects and can inhibit melanin synthesis. 4-Ethylresorcinol has potential whitening value.

Acenocoumarol (Standard) is the analytical standard of Acenocoumarol. This product is intended for research and analytical applications. Acenocoumarol is an anticoagulant that functions as a Vitamin K antagonist. Acenocoumarol inhibits MAPK/ERK/JNK signaling pathway, reduces the nuclear translocation of NF-κB p65, activates Akt/GSK3β signaling pathway. Acenocoumarol induces apoptosis in cell A549, arrests cell cycle at S phase.

FGIN 1-27 (Standard) is the analytical standard of FGIN 1-27 (HY-101059). This product is intended for research and analytical applications. FGIN-1-27 is a blood-brain barrier-penetrant TSPO ligand with a K_i value of 5 nM. FGIN 1-27 inhibits PKC-β, PKA/CREB, p38/ERK MAPK, MITF, tyrosinase, TRP-1, and TRP-2, thereby inhibiting melanogenesis and pigmentation. FGIN-1-27 alleviates X-ray radiation-induced astrocyte mitochondrial hyperfunction, reduces ROS and superoxide production, inhibits excessive activation of A1-type astrocytes, downregulates GFAP and C3 protein expression, and restores astrocyte proliferative capacity. FGIN-1-27 produces anticonvulsant effects in normal mice; in diazepam-withdrawn mice, the brain MDR pathway becomes subsensitive, and the anticonvulsant activity disappears. FGIN-1-27 attenuates pigmentation in zebrafish embryos and ameliorates UVB-induced skin pigmentation in guinea pigs. FGIN-1-27 directly stimulates testicular Leydig cells while upregulating luteinizing hormone levels, causing an acute increase in serum testosterone in male rats. FGIN 1-27 can be used for research related to hyperpigmentation, epilepsy, brain injury, and other diseases.

H-89 dihydrochloride (Standard) is the analytical standard of H-89 dihydrochloride (HY-15979A). This product is intended for research and analytical applications. H-89 dihydrochloride is a potent and selective inhibitor of protein K_inase A (PKA) with an IC₅₀ of 48 nM and has weak inhibition on PKG, PKC, Casein K_inase.

The Anti-TEM7R/PLXDC2 Antibody is a human-derived antibody expressed in CHO cells, targeting TEM7R/PLXDC2. The Anti-TEM7R/PLXDC2 Antibody contains a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for the Anti-TEM7R/PLXDC2 Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).

HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models.

AP736 is a potent tyrosinase inhibitor (IC₅₀ = 0.9 μM) with anti-melanogenesis activity in normal human melanocytes (IC₅₀ = 0.11 μM). AP736 suppresses the expression of tyrosinase and TRP-1/2 by inhibiting the cAMP-PKA-CREB signalling axis, leading to reduced microphthalmia-associated transcription factor (MITF) transcripts and proteins. AP736 can be used for melanogenesis and hyperpigmentation research.

HA-100 (Standard) is the analytical standard of HA-100 (HY-100984). This product is intended for research and analytical applications. HA-100 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 also used as a ROCK inhibitor.

Linderane (Standard) is the analytical standard of Linderane (HY-N0688). This product is intended for research and analytical applications. Linderane is an orally active natural sesquiterpene lactone with blood-brain barrier permeability. Linderane indirectly activates PDE3 by activating ERK/STAT3, thereby inhibiting the cAMP/PKA/CREB signaling pathway and hepatic gluconeogenesis. Linderane protects pancreatic β cells against oxidative damage by inhibiting the activation of the p38 MAPK pathway and activating the Nrf2 pathway. Linderane inhibits cell apoptosis and ameliorates intestinal mucosal inflammation by suppressing the IL-6/JAK/STAT3 signaling pathway. Linderane reduces pain sensitivity and alleviates anxiety-like behaviors by activating cannabinoid receptor 2 (CB2R). Linderane can be used in studies related to type 2 diabetes, ulcerative colitis, and chronic inflammatory pain with anxiety.

Antifungal agent 140 (compound 5p) is a potent antifungal agent with broad-spectrum antifungal activity. Antifungal agent 140 exerts a dual mechanism by targeting the Ras/cAMP/PKA pathway to inhibit hyphal formation and the ergosterol biosynthesis pathway. Antifungal agent 140 enhances survival, reduces fungal load in the kidneys, and strengthens host immune responses in a murine model of systemic candidiasis. Antifungal agent 140 can be used for research of resistant fungal infections.

Acenocoumarol-d₅ is the deuterium labeled Acenocoumarol (HY-B1014). Acenocoumarol is an anticoagulant that functions as a Vitamin K antagonist. Acenocoumarol inhibits MAPK/ERK/JNK signaling pathway, reduces the nuclear translocation of NF-κB p65, activates Akt/GSK3β signaling pathway. Acenocoumarol induces apoptosis in cell A549, arrests cell cycle at S phase.

PKA/AKAP-IN-2 (15109) is a non-peptide inhibitor of the interaction between protein kinase A (PKA) and A kinase anchoring proteins (AKAP). PKA/AKAP-IN-2 can be utilized in research related to cAMP disturbance associated diseases.

Sitagliptin (MK-0431) phosphate monohydrate (Standard) is the analytical standard of Sitagliptin phosphate monohydrate (HY-13749B). This product is intended for research and analytical applications. Sitagliptin phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin phosphate monohydrate 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 phosphate monohydrate 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 phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes.

4-Cyano-3-methylisoquinoline is an inhibitor for protein kinase A (PKA) with an IC₅₀ of micromolar level. 4-Cyano-3-methylisoquinoline reverses morphine tolerance in mouse model.

PKA/AKAP-IN-1 (compound 15126) is a non-peptide inhibitor of the interaction between protein kinase A (PKA) and A kinase anchoring proteins (AKAP). PKA/AKAP-IN-1 can be utilized in research related to cAMP disturbance associated diseases.