h9c2

EUK-134, a synthetic superoxide dismutase (SOD) catalase mimetic, exhibits potent antioxidant activities and inhibits the formation of β-amyloid and related amyloid fibrils.

Gadolinium chloride is a calcium-sensing receptor (CaSR) agonist

Nilotinib (AMN107) is a Bcr-Abl tyrosine kinase inhibitor with oral activity. Nilotinib has antitumor activity and may be used for the treatment of Imatinib-resistant chronic myelogenous leukemia (CML).

CLT-28643 is a potent and specific α5β1-Integrin inhibitor that prevents fibrosis in glaucoma filtration surgery (GFS), inhibits tumor growth and angiogenesis, suppresses fibrosis and inflammation in a bleomycin-induced lung fibrosis model, and improves insulin sensitivity and cardiac function in H9C2 cells from obese mice.

Moracin O shows significant neuroprotective, and analgesic activities, it also has a strong protective influence against doxorubicin-induced cardiomyopathy in H9c2 cells with the EC50 value of 4.5 ± 1.3 μM. Moracin O exhibits potent in vitro inhibitory ac

Ladanetin-6-O-β-(6′′-O-acetyl)glucoside, a flavonoid extracted from Dracocephalum tanguticum whole plants, exhibits antioxidant properties and cardioprotective effects, mitigating Doxorubicin-induced toxicity in H9c2 cells [1].

Regaloside C, a glycerol glucoside isolated from the Lilium genus, exhibits notable anti-inflammatory properties.

Pedaliin 6''-acetate (compound 10), a natural product from Dracocephalum tanguticum, demonstrates antioxidative properties and cytoprotective effects against doxorubicin (DOX)-induced toxicity in H9c2 cardiomyocytes, with an EC50 of 19.1 μM [1].

Nrf2 HO-1 Activator 3 (Compound C3a) is an activator of the Nrf2 signaling pathway that facilitates the translocation of Nrf2 into the nucleus and enhances the expression of heme oxygenase-1 (HO-1). In H9c2 cardiomyocytes subjected to H2O2 or high glucose stimulation, Nrf2 HO-1 Activator 3 inhibits the excessive expression of ROS and MDA, suppressing cell viability and colony formation, thereby exhibiting antioxidant activity.

AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway[1][2][3]. Treatment with 100 μM Zidovudine (AZT) for 48h disrupts the mitochondrial tubular network via accumulation of AZT triphosphate (AZT-TP) in H9c2 cells. AZT triphosphate accumulation causes downregulation of Opa1 and upregulation of Drp1. AZT triphosphate causes mitochondrial dysfunction, increases the production of cytotoxic reactive oxygen species (ROS), and impairs the balance of the mitochondrial quality control system in H9c2 cell model established from rat embryonic myoblasts[1]. [1]. Ryosuke Nomura, et al. Azidothymidine-triphosphate Impairs Mitochondrial Dynamics by Disrupting the Quality Control System. Redox Biol. 2017 Oct;13:407-417. [2]. Takeya Sato, et al. Engineered Human tmpk/AZT as a Novel Enzyme/Prodrug Axis for Suicide Gene Therapy. Mol Ther. 2007 May;15(5):962-70. [3]. K Y Hostetler, et al. Enhanced Oral Absorption and Antiviral Activity of 1-O-octadecyl-sn-glycero-3-phospho-acyclovir and Related Compounds in Hepatitis B Virus Infection, in Vitro. Biochem Pharmacol. 1997 Jun 15;53(12):1815-22.

1. Nardosinone has inhibitory effect on Ang II-induced hypertrophy in H9c2 cells, might be mediated by targeting PI3K Akt and MEK ERK signaling pathways. 2. Nardosinone could protect against the neuronal injury exposed to OGD, which may be relevant to the

Randialic acid B shows significant cell-protective effects against H2O2-induced H9c2 cardiomyocyte injury.

N-Desbutyl dronedarone is an active metabolite of the antiarrhythmic agent dronedarone .1,2,3It is formed from dronedarone by cytochrome P450s (CYPs) and monoamine oxidase (MAO) in human hepatocyte preparations.4N-Desbutyl dronedarone inhibits the binding of 3,3',5-triiodo-L-thyronine to the thyroid hormone receptors TRα1and TRβ1(IC50s = 59 and 280 μM for the chicken and human receptors, respectively).1It inhibits CYP2J2-mediated formation of 14,15-EET from arachidonic acid and soluble epoxide hydrolase-mediated formation of 14,15-DHET from 14,15-EET (IC50s = 1.59 and 2.73 μM, respectively, in cell-free assays).2N-Desbutyl dronedarone decreases intracellular ATP levels in H9c2 rat cardiomyocytes (IC50= 1.07 μM) and inhibits mitochondrial complex I, also known as NADH dehydrogenase, and mitochondrial complex II, also known as succinate dehydrogenase, activities in isolated rat heart mitochondria (IC50s = 11.94 and 24.54 μM, respectively).3 1.Van Beeren, H.C., Jong, W.M.C., Kaptein, E., et al.Dronerarone acts as a selective inhibitor of 3,5,3'-triiodothyronine binding to thyroid hormone receptor-α1: in vitro and in vivo evidenceEndocrinology144(2)552-558(2003) 2.Karkhanis, A., Tram, N.D.T., and Chan, E.C.Y.Effects of dronedarone, amiodarone and their active metabolites on sequential metabolism of arachidonic acid to epoxyeicosatrienoic and dihydroxyeicosatrienoic acidsBiochem. Pharmacol.146188-198(2017) 3.Karkhanis, A., Leow, J.W.H., Hagen, T., et al.Dronedarone-induced cardiac mitochondrial dysfunction and its mitigation by epoxyeicosatrienoic acidsToxicol. Sci.163(1)79-91(2018) 4.Klieber, S., Arabeyre-Fabre, C., Moliner, P., et al.Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drugPharmacol. Res. Perspec.2(3)e00044(2014)

Bisoprolol, a selective beta-1 adrenergic receptor antagonist, selectively and competitively binds to and blocks beta-1 adrenergic receptors in the heart, thereby with antihypertensive activity and devoid of intrinsic sympathomimetic activity.

CDK8-IN-7 (compound 12) is a potent and selective inhibitor of cyclin-dependent kinase 8 (CDK8), with a Kd of 3.5 nM, and has demonstrated potential for AML-cancer research.

CDK8-IN-6 (compound 9) is a potent inhibitor of cyclin-dependent kinase 8 (CDK8) with a Kd of 13 nM, demonstrating significant research potential in AML cancers.

INF 195 is an inflammasome NLRP3 inhibitor that inhibits NLRP3-driven macrophage pyroptosis and IL-1β release. INF 195 reduces isoproterenol-induced hypertrophy in H9c2 rat myoblasts and can be used to study myocardial ischemia and myocardial infarction.

Bisoprolol is a cardioselective β1-adrenergic blocker used for secondary prevention of heart failure, myocardial, angina pectorisinfarction (MI) and mild to moderate hypertension.

Cinnamyl caffeate has cardiovascular protective effects, it can increase H9c2 cellular antioxidant potential, decrease intracellular calcium ion ([Ca2+]i) level, and prevent cell apoptosis; it possesses potent antiproliferative activity with the EC(50) value of 0.114 microM, toward colon 26-L5 carcinoma. Cinnamyl caffeate possesses potent NO inhibitory activity with the IC(50) value of 9.53 microM.