hypertrophy

Indapamide (Noranat) is a non-thiazide sulphonamide diuretic compound, generally used in the treatment of hypertension, as well as decompensated cardiac failure.

Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM). Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent.

Syringin (eleutheroside-b) is a compound with antitumor, antiproliferative, immunomodulatory and platelet aggregation inhibiting effects.

Tamarixetin (4'-O-Methyl Quercetin) is a natural flavonoid derivative of quercetin that exhibits anti-inflammatory and antioxidative effects, offering protection against cardiac hypertrophy.

20-HETE promotes cell proliferation and migration in cancer and can be used to study prostate tumors and cardiac hypertrophy by activating the protein kinase C pathway to increase FBXO10 expression.

Enrasentan (sb-217242) is a mixed antagonist of ET(A) and ET(B) receptors that reduces blood pressure, prevents cardiac hypertrophy, and protects myocardial function.

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Prazosin hydrochloride (Vasoflex) reduces peripheral resistance and relaxes vascular smooth muscles as a selective adrenergic alpha-1 antagonist by a mechanism not completely known. Prazosin hydrochloride is a synthetic piperazine derivative with hypotensive antiadrenergic properties, It is used in the treatment of heart failure, hypertension, pheochromocytoma, Raynaud's syndrome, prostatic hypertrophy, and urinary retention.

Phenylethyl isothiocyanate (JC5411) is an HDAC inhibitor. It potentially for the treatment of benign prostatic hypertrophy.

Trimethylamine N-oxide dihydrate (TMANO dihydrate) is a gut microbiota-dependent metabolite derived from dietary choline and other trimethylamine-containing nutrients. It induces inflammation by activating the ROS/NLRP3 inflammasome and promotes fibroblast differentiation and cardiac fibrosis via the TGF-β/Smad2 signaling pathway. TMANO dihydrate can be used to establish models of cardiac hypertrophy and cardiac fibrosis.

Methyl retinoate (Retinoic acid, methyl ester) induces aseptic inflammation at the site of administration in in vivo experiments, which causes an increase in the number of leukocytes in the blood and a decrease in the levels of red blood cells and Hb.Methyl retinoate promotes spontaneous leukemia.Methyl retinoate can be Used in the treatment of gastric hypertrophy and ulcers due to vitamin A deficiency. Translated with www.DeepL.com/Translator (free version)

L002, a potent, cell-permeable, reversible, and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM, directly binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain. By blocking histone acetylation, p53 acetylation, and STAT3 activation, L002 shows potential in the treatment of hypertension‐induced cardiac hypertrophy and fibrogenesis.

Pterosin B, a type of indanone found in Pteridium aquilinum, is an inhibitor of salt-induced kinase 3 (Sik3) signal transduction. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice by inhibiting Sik3.

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.

Enrasentan (also known as SB-217242) is a dual receptor endothelin antagonist with a higher affinity for the ET(A) receptor. In animal models of hypertension and cardiac hypertrophy, this compound reduces blood pressure, prevents cardiac hypertrophy, and preserves myocardial function. Enrasentan enhances survival rates, limits left ventricular remodeling, and maintains myocardial performance in hypertensive cardiac hypertrophy and dysfunction.

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.

JZ19 reduces intracellular levels of LDH and ROS and demonstrates antioxidant activity against oxygen-glucose deprivation (OGD)-induced myocardial cell damage. It reverses Isoproterenol-induced myocardial cell hypertrophy and apoptosis through the PI3K-AKT-GSK3β signaling pathway. Additionally, JZ19 alleviates Isoproterenol-induced heart failure in mouse models.

Delocamten is an inhibitor of cardiac myosin, with an IC50 value of 1.1 μM. It is useful in research on hypertrophic cardiomyopathy, left ventricular hypertrophy, and diastolic dysfunction.

Phosphodiesterase-IN-2 (Compound C7) is an orally active and selective inhibitor of phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. It enhances hepatic microsomal stability and reduces blood-brain barrier permeability. Phosphodiesterase-IN-2 exhibits favorable pharmacokinetic properties in mouse models and can alleviate isoprenaline-induced cardiac hypertrophy.

ZAK-IN-1 is an orally active and selective inhibitor of the leucine zipper and sterile-alpha motif kinase ZAK, with an IC50 of 4 nM and a KD of 8 nM. It demonstrates exceptional selectivity against 403 types of wild-type kinases. ZAK-IN-1 effectively blocks the p38/GATA-4 and JNK/c-Jun signaling pathways, significantly suppressing cardiac hypertrophy. This compound is applicable in the study of hypertrophic cardiomyopathy (HCM).

IHMT-15130 is a potent and irreversible BMX kinase inhibitor (IC50=1.47 nM). It suppresses the secretion of inflammatory cytokines, obstructs inflammatory signaling pathways, and alleviates angiotensin II-induced myocardial hypertrophy in mice. IHMT-15130 shows potential for research in myocardial hypertrophy.

AH001 is an orally active compound that binds to a concealed pocket near GDP within RhoA, exhibiting a binding affinity of 73.16 nM. By interacting with GDP, AH001 stabilizes the interaction between RhoA and its endogenous inhibitor, RhoGDIα. This compound reduces nuclear translocation of downstream MRTFA and downregulates fibrosis/hypertrophy-related proteins. AH001 alleviates myocardial remodeling in various heart failure animal models and 3D cardiac tissue models. Its cardioprotective effects are mediated through the RhoA-RhoGDIα axis, effectively inhibiting downstream RhoA activation signals.

SGLT2-IN-2 (Compound E9) is an inhibitor of SGLT2 and significantly enhances the inhibition of SGLT2, NHE1, and SOD enzyme activities. It provides protection against myocardial cell damage induced by glucose-free DMEM. Additionally, SGLT2-IN-2 markedly improves cardiac function in TAC-induced heart failure (HF) mice, suppressing myocardial cell hypertrophy and collagen deposition. It reduces myocardial tissue damage and boosts autophagy in damaged myocardial cells, increasing the survival rate of HF mice.