cardiovascular research

KDM4-IN-4 (compound 47) is a potent inhibitor of histone lysine demethylase 4 (KDM4), with a binding constant of approximately 80 μM for the KDM4A-Tudor domain. It inhibits H3K4Me3 binding to the Tudor domain in cellular contexts with an EC50 value of 105 μM, holding potential for anticancer research applications [1].

AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid and a potent, selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). By blocking the production of arachidonate and 12-hydroxyeicosatetraenoic acid in calcium ionophore-challenged platelets, AACOCF3 hinders their synthesis. Additionally, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets, making it promising for cardiovascular disease research.

C-Myc Inhibitor 7, serving as both a c-Myc inhibitor and a multi-target protein degrader, effectively degrades proteins c-MYC, CK1α, GSPT1, and IKZF1 2 3 across various tumor cell types. It holds potential for research into diseases associated with high c-Myc expression, including cancer, cardiovascular and cerebrovascular conditions, and viral infections.

PF-07328948 is a branched-chain keto acid dehydrogenase kinase (BDK) inhibitor, useful in research on cardiovascular disease (CVD) and metabolic disorders.

AICAR (Acadesine) is an AMPK activator. AICAR has the functions of metabolic regulation, muscle function regulation, anti-cancer effect, neuroprotection and anti-aging.

Indazole is also called benzpyrazole or isoindazone. Its derivatives exhibit a wide range of biological activities. Indazole and its derivatives can be used in the research of cancer, neurological diseases, cardiovascular diseases, and gastrointestinal diseases.

D-fructose-1,6-diphosphate (D-fructose-1,6-diphosphate), also known as Fosfructose, is a cytoprotective natural sugar phosphate. It functions by promoting anaerobic glycolysis, which generates adenosine triphosphate (ATP) under ischemic conditions. This compound holds potential for research in cardiovascular ischemia, sickle cell anemia, and asthma.

Solenopsin HCl is an alkaloid extracted from fire ants, inhibiting phosphoinositide 3-kinase signaling and angiogenesis in a dose-dependent manner, affecting cardiovascular function, and used in cardiovascular disease research.

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.

GYKI-47261 dihydrochloride is an orally active and selective AMPA receptor antagonist, also a CYP2E1 inducer with broad anticonvulsant and neuroprotective activity, used in neurological and cardiovascular research.

KRH102140 is a PHD2 activator that reduces angiogenesis by inhibiting HIF-1alpha, used in cardiovascular disease research.

(E)-NMac1 is a compound extracted from Java ginger, useful in cardiovascular disease and neurodegenerative disease research.

BRD4-BD1-IN-2 is a selective and potent BRD4-BD1 inhibitor with an IC50 value of 2.51 µM, exhibiting 20-fold greater inhibitory activity against BRD4-BD1 compared to BRD4-BD2. [BRD4-BD1-IN-2] is applicable for research in cardiovascular and cancer-related diseases.

CB1 antagonist 1 is a CB1 receptor antagonist, used in the research of obesity and metabolic syndrome, neuroinflammatory disorders, cognitive disorders, and gastrointestinal disorders, psychosis, and cardiovascular.

Etamicastat can be used in the research of cardiovascular diseases. Etamicastat (BIA 5-453) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM.

TXNIP-IN-1 is an inhibitor of the TXNIP-TRX complex and used in the research of TXNIP-TRX complex associated metabolic disorder (diabetes), cardiovascular disease, or inflammatory disease.

Bimoclomol is a heat shock protein co-inducer employed in cardiovascular disease research.

AVE3085 is an endothelial nitric oxide synthase enhancer that restores endothelial function and reduces blood pressure in spontaneously hypertensive rats, used in cardiovascular disease research.

MeIm (compound 7), a peptide mimetic targeting PCSK9, exhibits cholesterol-lowering properties by enhancing the cellular uptake of LDL (EC 50 = 6.04 μM) and obstructing PCSK9's interaction with LDLR (IC 50 = 11.2 μM). This compound is useful for research in cardiovascular diseases.

PCSK9-IN-30 (Compound 3f), a PCSK9 inhibitor, effectively targets a cryptic binding groove on PCSK9, thereby preventing PCSK9 from associating with the low-density lipoprotein receptor (LDLR) (IC 50 = 537 nM). This inhibition aids in the restoration of low-density lipoprotein (LDL) uptake by liver cells and significantly reduces plasma cholesterol levels. Demonstrating good bioavailability in mice, PCSK9-IN-30 holds potential for research within cardiovascular disease contexts.

5-HT2A 5-HT2C inverse agonist 1 serves as a dual and potent inverse agonist for the 5-HT2A and 5-HT2C receptors, with hERG inhibition properties that mitigate cardiovascular risks. Demonstrating significant antipsychotic efficacy in the MK-801-induced mouse model, this compound holds potential for psychosis research.

7030B-C5, a PCSK9 inhibitor (IC50=1.61 μM), effectively reduces plasma cholesterol and triglyceride (TG) levels in vivo, thereby slowing the progression of atherosclerosis. This compound is used in research related to cardiovascular diseases.

BRD8518, a PCSK9 inhibitor (EC50=0.23 μM), effectively lowers lipid levels by upregulating LDLR expression and enhancing the uptake of LDL. This compound is utilized in cardiovascular disease research.

JW-65 (compound 20) is an inhibitor of TRPC3. It is utilized in research related to neurological and cardiovascular diseases.