cardiac diseases

ROCK-IN-5 (compound I-B-37) is a potent inhibitor of protein kinases, including ROCK, ERK, GSK, and AGC. ROCK-IN-5 exhibits the potential for cardiac, proliferative and neurodegenerative diseases research.

AM-8123 is an orally available nonpeptide APJ agonist.AM-8123 reduces collagen load and improves cardiac function. AM-8123 ameliorates myocardial infarction in rats and can be used to study cardiovascular diseases such as heart failure.

Examorelin (Hexarelin) is an agonist of growth hormone-releasing factor (GHRF), and for the treatment of cardiac diseases.

GSK-114, a selective inhibitor of TNNI3 Interacting Kinase (TNNI3K) with IC50 of 25 nM, shows significant bias for TNNI3K over B-Raf with IC50 of 1000 nM, exceptional broad spectrum kinase selectivity and adequate oral exposure to enable its use in cellul

Digoxigenin, a therapeutic drug belonging to the group of cardiac glycosides, is widely used in the management of congestive heart failure and other cardiac diseases

Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation of the cAMP pathway. Via generating a transcriptionally active complex with β-catenin, CREB acts as a mediator of Wnt signaling.ICG-001 is an inhibitor of β-catenin/CREB mediated transcription. The direct cellular target of ICG-001 is CREB. the inhibitory IC50of ICG-001 against β-catenin/CREB mediated transcription was 3 μM. ICG-001 treatment at the concentration of 25 μM for 24h significantly increased caspase activity in both colon cancer cell lines SW480 and HCT116 cell lines but not in normal colonic epithelial cells CCD-841Co. In a cell growth inhibition assay, the IC50s of ICG-001 against SW480 and HCT116 cells were 4.43 μM and 5.95 μM, respectively.In a SW620 nude mouse xenograft model, an water-soluble analog of ICG-001 given at the dose of 150 mg/kg i.v. once in every 2 days dramatically suppressed tumor growth. In a bleomycin-induced pulmonary fibrosis mice model, ICG-001 given at the dose of 5 mg/kg per day reversed pulmonary fibrosis. In a rat myocardial infarction model, ICG-001 was administrated subcutaneously at the dose of 50 mg/kg/day for 10 days which significantly improved cardiac contractile function after myocardial infarction in the rats.

TRPM4-IN-1 (4-chloro-2-(2-(2-chlorophenoxy)acetamido)benzoic acid) is a potent and selective inhibitor of TRPM4 with an IC50 of 1.5 μM.

Mitochonic acid 5 (MA-5) is a derivative of the plant hormone indole-3-acetic acid. Mitochonic acid 5 binds mitochondria and ameliorates renal tubular and cardiac myocyte damage.It has been shown to improve survival of fibroblasts from patients with mitochondrial diseases.