cardiomyocyte

BTZO-1 is an antioxidant response element (ARE) activator with cardioprotective activity.

KY02111 facilitates differentiation of hPSCs to cardiomyocytes by inhibiting Wnt signaling, maybe affect downstream of GSK3β and APC.

Cyclic somatostatin (SRIF-14) is a cyclic tetradecapeptide that regulates various endocrine and nervous system functions.

Gue1654 is a selective OXE-R inhibitor that attenuates coronary artery ligation-induced ischemic myocardial injury and cardiomyocyte oxygen/glucose deprivation-induced injury in mice through activation of BCAT1.Gue1654 inhibits OXE-R-inhibited protein kinase C-ε (PKC-ε)/nuclear factor κB (NF-κB) signaling and apoptosis in cardiomyocytes. Gue1654 can be used to study cardiovascular disease.

ML-9 suppresses MLCK, PKA, and PKC activity with Ki values of 4, 32, and 54 μM, respectively. ML-9 is a selective and effective inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK), and stromal interaction molecule 1 (STIM1) activity. ML-9 causes autophagy by stimulating autophagosome formation and inhibiting their degradation.

VUT-MK142 is a new cardiomyogenic small molecule promoting the differentiation of pre-cardiac mesoderm into cardiomyocytes,which may be useful to differentiate stem cells into cardiomyocytes for cardiac repair.

Pterosin B is a salt-inducible kinase 3 (Sik3) signaling inhibitor widely found in leaves and shoots of green plants.Pterosin B promotes the expression of G6pc, protects against Ang II-induced cardiomyocyte hypertrophy, and acts through the regulation of the expression level of NAD(P)H oxidase 2/4.

ERBB agonist-1 (Compound EF-1) is an ERBB4 agonist that activates the ERBB4 signaling pathway by inducing ERBB4 receptor dimerization, with an EC50 of 10.5 μM. It promotes phosphorylation of Akt and ERK1 2, reduces collagen expression in cardiac fibroblasts, and inhibits H2O2-induced cardiomyocyte death and Ang II-induced cardiac hypertrophy. Furthermore, ERBB agonist-1 can prevent myocardial fibrosis and demonstrates cardioprotective effects in mouse models.

Lipoxygenin is an inhibitor of 5-lipoxygenase (5-LO) with an IC50value of 5 μM for inhibition of 5-LO product synthesis in isolated human granulocytes stimulated with the cation ionophore A23187 .1It inhibits hedgehog-dependent signaling in Shh-LIGHT2 cells and TGF-β-, activin A-, bone morphogenic protein (BMP)-, or Wnt-dependent signaling in HEK293T cells (IC50s = 9.3, 3.2, 8.2, 9.6, and 3.7 μM, respectively, in luciferase reporter assays). Lipoxygenin (5 and 10 μM) increases levels of troponin T (TnnT), a marker of cardiomyocyte differentiation, in human induced pluripotent stem cells (iPSCs) stimulated with BMP4 and the glycogen synthase kinase 3 (GSK3) inhibitor CHIR99021 .

Brain Natriuretic Peptide (1-32), rat acetate (BNP (1-32), rat acetate) is a 32-amino acid polypeptide hormone synthesized by ventricular cardiomyocytes in response to myocardial cell stretching (cardiomyocyte distension)[1].

GRKs-IN-1 hydrochloride, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=130 nM) and GRK5 (IC50=7.1 μM).GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine[1]. [1]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):3052-3069.

Cutamesine dihydrochloride (SA4503 dihydrochloride) is a selective σ1 receptor agonist (IC50: 17.4 nM). It shows selectivity for σ1 over σ2 receptors, and inhibits angiotensin II-induced cardiomyocyte hypertrophy in vitro and attenuates myocardial hypertrophy in vivo. In a rat model of experimental stroke, it enhances brain plasticity and sensorimotor function.

17R(18S)-EpETE is an oxylipin and a cytochrome P450 metabolite of eicosapentaenoic acid .1,217R(18S)-EpETE is an activator of large-conductance calcium-activated potassium (BKCa) channels, increasing the potassium current amplitude by 15-fold in isolated rat cerebral artery vascular smooth muscle cells (VSMCs) at +60 mV when used at a concentration of 50 nM.2It has negative chronotropic effects in isolated neonatal rat cardiomyocytes (NRCMs; EC50= ~1-2 nM) and prevents calcium-induced increases in the spontaneous beating of NRCMs.3,4 1.Schwarz, D., Kisselev, P., Ericksen, S.S., et al.Arachidonic and eicosapentaenoic acid metabolism by human CYP1A1: Highly steroselective formation of 17(R), 18(S)-epoxyeicosatetraenoic acidBiochem. Pharmacol.67(8)1445-1457(2004) 2.Lauterbach, B., Barbosa-Sicard, E., Wang, M.H., et al.Cytochrome P450-dependent eicosapentaenoic acid metabolites are novel BK channel activatorsHypertension39(2 Pt. 2)609-613(2002) 3.Falck, J.R., Wallukat, G., Puli, N., et al.17(R),18(S)-Epoxyeicosatetraenoic acid, a potent eicosapentaenoic acid (EPA) derived regulator of cardiomyocyte contraction: Structure-activity relationships and stable analoguesJ. Med. Chem.54(12)4109-4118(2011) 4.Arnold, C., Markovic, M., Blossey, K., et al.Arachidonic acid-metabolizing cytochrome P450 enzymes are targets of omega-3 fatty acidsJ. Biol. Chem.285(43)32720-32733(2010)

2'-Deoxyadenosine-5'-triphosphate (Deoxyadenosine 5-triphosphate) (dATP) is a naturally occurring small molecule nucleotide used in cells for DNA synthesis or replication. 2'-Deoxyadenosine-5'-triphosphate (dATP) is a substrate for DNA polymerase. 2'-Deoxyadenosine-5'-triphosphate (dATP) is an inhibitor of RNA through an inactive alpha4beta4 quaternary structure. Deoxyadenosine-5'-triphosphate inhibits RNA through the inactive α4beta4 quaternary structure.2'-Deoxyadenosine-5'-triphosphate has been associated with cardiomyocyte growth.

DMX-5804 is a potent, selective MAP4K4 inhibitor, with an IC50 of 3 nM.DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.

FC9402 is a potent and selective inhibitor of sulfide quinone oxidoreductase (SQOR), which can be used to regulate cardiovascular conditions by reducing cardiomyocyte hypertrophy and left ventricle (LV) fibrosis induced by TAC [1].

CCG-271423 is a potent and selective inhibitor of GRK5, demonstrating activity against GRK5 (IC50: 0.0021 μM) and GRK2 (IC50: 44 μM); it reduces Ca2+ transients and inhibits cardiomyocyte contractility.

WLSEAGPVVTVRALRGTGSW TFA, a cardiomyocyte-specific peptide, exhibits enhanced performance through its expression in exosomes, which notably improves uptake by cardiomyocytes, reduces apoptosis within these cells, and increases cardiac retention after intramyocardial injection in vivo [1] [2].

SDF-1α (human) serves as a chemotactic agent for mononuclear cells through its interaction with the CXCR4 receptor, facilitating critical biological processes such as stem cell homing, retention, survival, and proliferation, in addition to cardiomyocyte repair, angiogenesis, and ventricular remodeling post-myocardial infarction. It holds significant utility in cardiovascular disease research [1] [2].

CDK-IN-11, a heterocyclic compound, promotes cardiomyocyte maturation [1].

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

Ac2-26, an annexin A1 mimetic peptide, was able to attenuate renal inflammatory injury in a diabetic mouse model through inhibition of p38MAPK/NF-κB, as well as sepsis-induced cardiomyocyte apoptosis through the LXA4/PI3K/AKT signalling pathway, and hepatic ischaemia-reperfusion injury in mice by modulating IL-22/IL-22R1/STAT3 signalling pathway.

TRV120027 TFA is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R) and engages ß-arrestins while blocking G-protein signaling.

TRV120027 is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1. TRV120027 inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility.