PKA Inhibitor

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.

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.