cardiac diseases

ROCK-IN-5 (compound I-B-37) is a potent inhibitor of protein kinases, including ROCK, ERK, GSK, and AGC, with potential applications in cardiac, proliferative, and neurodegenerative disease 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.

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

SIRT3 Activator 1 (Compound 5v) is a selective activator of SIRT3. It enhances the expression of SIRT3, leading to upregulation of SOD2 and OPA1. This activity effectively mitigates mitochondrial dysfunction, alleviates oxidative stress, and maintains the vitality of cardiac myocytes. SIRT3 Activator 1 is useful in the study of cardiovascular diseases.

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

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

Cyclic GMP is an endogenous second messenger that initiates interferon production in response to cytoplasmic DNA. It activates the stimulator of interferon genes (STING), triggering a signaling cascade that results in the production of type I interferons and other immune mediators. The conjugate of cyclic GMP and AMP, known as Cyclic-GMP-AMP, can induce the phosphorylation and nuclear translocation of IRF3, thereby enhancing antiviral immune responses. Additionally, Cyclic GMP may activate PDE to degrade cAMP, inhibit the myocardial calcium current ICa, and regulate cardiac contractility. The derivative 8-Br-cGMP exhibits antiplatelet activity, and Cyclic GMP is used in research related to antiviral immunity and cardiovascular diseases.

Enlicitide chloride is an effective PCSK9 antagonist. It is utilized in the research of cardiovascular diseases such as atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or associated cardiovascular and cardiac metabolic disorders.

Skeletal muscle-targeted peptide MSP, a muscle-targeting peptide (MTP) composed of seven amino acids (ASSLNIA), selectively binds to various ligands in muscle tissues. This targeting capability makes it a useful tool in researching cardiac and skeletal muscle diseases.

BDK-IN-1 (compound (-)-43) is a BDK inhibitor with an IC50 of 0.23 μM and a maximum inhibition rate of 90%. It reduces phosphorylated-E1 levels and is useful in the study of cardiac metabolic diseases.

AM-001 is a non-competitive inhibitor of Epac1, preventing the activation of its downstream effector Rap1 in cultured cells. This compound is utilized in research related to cardiac diseases.

HYNIC-CTP is a conjugate of HYNIC and CTP (cardiac-targeting peptide). It acts as a chelator, allowing HYNIC to bind with the radioisotope 99mTc, resulting in the formation of 99mTc-HYNIC-CTP. This compound is specifically absorbed by the heart, facilitating cardiac imaging and thereby aiding in the research of heart diseases.

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.

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.

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.