hypertrophic

Aficamten is a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy.

Trapencaine is a newly synthesized carbamate type local anesthetic that induces conformational changes in sodium channels on hypertrophic cell membranes.

Trans-Tranilast is an antiallergic drug developed by Kissei Pharmaceuticals. It was approved in 1982 for use in Japan and South Korea for bronchial asthma. Indications for keloid and hypertrophic scar were added in 1993. It has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.

Methyl Aminolevulinate Hydrochloride (5-Aminolevulinic acid methyl ester) is commonly used in photosentizer reagents for photodynamic therapy to treat conditions such as Acne vulgaris and hypertrophic scarring.

Fropofol (2-fluoro-1,3-diisopropylbenzene) is a non-anesthetic small molecule that specifically reduces myocardial contractility and inhibits myofilament contraction. It can be used in research on hypertrophic cardiomyopathy and cardiovascular diseases.

JNJ-28330835 is a non-steroidal, oral selective androgen receptor modulator (SARM). In assays using androgen-responsive cells, JNJ-28330835 exhibits both agonist and antagonist activity. JNJ-28330835 acts as an agonist for markers of both osteoclast and osteoblast activity, thereby reducing bone turnover.

GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.GATA4-NKX2-5-IN-1  dose-dependently inhibits the GATA4–NKX2-5 tran

ST2-IN-1 (compound 31) is an inhibitor of Stimulation-2 (ST2) with an IC50 of 7 μM in AlphaLISA assays and 7.19 μM in HEK-Blue assays. This compound effectively attenuates the ST2/IL-33 signaling pathway in human hypertrophic cells.

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.

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).

(±)-Desisopropylpropranolol (N-Desisopropylpropranolol) is a metabolite of Propranolol. Propranolol acts as a non-selective β-adrenergic receptor (βAR) antagonist with high affinity for both β1AR and β2AR, having Ki values of 1.8 nM and 0.8 nM, respectively. It inhibits the binding of [3H]-DHA to rat brain membrane preparations with an IC50 of 12 nM. Propranolol is used in studies related to hypertension, pheochromocytoma, myocardial infarction, arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.

Myosin-IN-2 (Example 16) is an inhibitor of Myosin ATPase, exhibiting an IC50 value of 1.06 μM. It is applicable in research related to cardiac diseases, including hypertrophic cardiomyopathy (HCM).

GRK5-IN-5 (Compound 4a) is a selective inhibitor of G protein-coupled receptor kinase 5 (GRK5) with an IC50 value of 0.03 μM. It shows an IC50 of 2.2 μM for GRK2 and 0.036 μM for GRK6. GRK5-IN-5 exhibits potent anti-hypertrophic activity in cardiac muscle and inhibits the proliferation of non-cardiac cells. It blocks pathological cardiac remodeling by inhibiting the abnormal upregulation of hypertrophic marker genes Nppa and Nppb. GRK5-IN-5 is useful for research in myocardial hypertrophy.

Myosin-IN-5 (Example 3) is a myosin inhibitor with an IC50 of 1.84 μM against bovine cardiac myosin. It demonstrates strong selectivity between cardiac and skeletal muscle myosins, exhibiting IC50 values of 43.4 μM for bovine cardiac myofibrils and 1.5 μM for rabbit skeletal muscle myofibrils. This compound is useful in researching hypertrophic cardiomyopathy (HCM).

Ethyl L-leucinate HCl has been used as a hypertrophic agent to monitor its effects on myotubes and has also been used as a component of PMG media for culturing yeast.

Cibenzoline is an antiarrhythmic agent that inhibits the KATP channel by directly affecting the pore-forming Kir6.2 subunit rather than the SUR1 subunit. Cibenzoline shows little anticholinergic activity. Cibenzoline markedly reduces LVPG which has a close relationship with myocardial contractility decreasing. Cibenzoline has the potential for hypertrophic obstructive cardiomyopathy research[1][2].

CCG-273463 is a potent, covalent, selective inhibitor of GRK5 (IC50: 9 nM). CCG-273463 can be used to study heart failure, hypertrophic cardiomyopathy and cancer.

JB062 is a chemical compound acting as a nonmuscle myosin inhibitor, exhibiting IC50 values of 1.6, 5.4, and >100 μM against skeletal muscle myosin, cardiac muscle myosin, and smooth muscle myosin II, respectively. It selectively exhibits cytotoxicity towards human cancer cells without affecting normal cells. The compound is applicable in research fields concerning muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy.

JB002, a myosin II inhibitor, exhibits potent activity with an IC50 of ≤10 μM. It holds potential for research applications in muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy.

Propranolol-D7 (ring-D7) is a deuterated form of Propranolol (TPL0294) hydrochloride, which is a non-selective β-adrenergic receptor (βAR) antagonist with high affinity for both β1AR and β2AR, having Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol (TPL0294) hydrochloride inhibits the binding of [3H]-DHA to rat brain membrane preparations with an IC50 of 12 nM. It is applicable in research related to hypertension, pheochromocytoma, myocardial infarction, arrhythmia, angina, and hypertrophic cardiomyopathy.

Momordicine I is a natural cucurbitane-type triterpene exhibiting antihypertensive, anti-inflammatory, anti-hypertrophic, anti-fibrotic, and antioxidant properties. Its mechanisms of action include regulating insulin signalling, inducing cancer cell apoptosis, and modulating NO, ACE, PI3K/Akt, NF-κB, Nrf2, c-Met/STAT3 pathways, and may be applied in cardiovascular diseases and inflammation.