dose-dependently

MCL0020 is a potent and selective melanocortin MC4 receptor antagonist (IC50 values are 11.63, 1115, and >10,000 nM at MC4, MC3, and MC1 receptors, respectively). It significantly reverses stress-induced anorexia without affecting food intake in free-feeding rats and exhibits anxiolytic-like activity in vivo.

Astragaloside IV (AS-IV), an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine.1 It dose-dependently inhibits human adenovirus type 3 (HAdV-3) in A549 cells (IC50 = 23 μM; LC50 = 865 μM).It inhibits replication of HAdV-3 and decreases HAdV-3-induced apoptosis. It has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems. In particular, it reduces myocardial infarct size in dogs when administered prior to coronary ligation and reduces reperfusion arrhythmias in isolated rat hearts.

Y1 receptor antagonist 1 (H 409-22 isomer) is the active isomer of H-409/22, a neuropeptide Y (NPY) Y1 receptor antagonist that dose-dependently antagonizes the vascular response to exogenous and endogenous NPY in pigs. lagodeoxycholic acid (H 409-22 isomer) is the active isomer of H-409/22, an antagonist of neuropeptide Y (NPY) Y1 receptor.

AA 2379 is an orally available antirheumatic agent with anti-inflammatory and antipyretic activity that dose-dependently inhibits complement-mediated yeast glycan-induced paw edema in rats and yeast glycan-activated serum-induced peritonitis in mice.

ABT-963 is a potent and selective inhibitor of disubstituted pyridazinone cyclooxygenase-2 (LOX2) that dose-dependently reduces injury perception in a carrageenan model of nociceptive sensitization.ABT-963 is used in the study of arthritis.

AMPK activator 4 is a potent and selective AMPK activator that does not inhibit mitochondrial complex I. It selectively activates AMPK in muscle tissue, dose-dependently improves glucose tolerance in normal mice, significantly reduces fasting glucose levels, and improves insulin resistance in db/db diabetic mice. [AMPK activator 4 has hypoglycemic effects.]

Ezurpimtrostat hydrochloride (GNS561 hydrochloride) is an orally available palmitoyl protein thioesterase-1 inhibitor with antifibrotic, antiviral, and anticancer effects that blocks cancer cell proliferation by interacting with palmitoyl protein thioesterase to inhibit late autophagy and dose-dependently increase lysosomal accumulation.

Litoxetine is a selective 5-HT uptake inhibitor and is a 5-HT3 receptor antagonist. Litoxetine acts as an antidepressant and has shown antiemetic properties in ferrets. Litoxetine (1 and 10 mg/kg i.v.) dose-dependently reduced the number of regurgitations and vomiting and delayed the onset of vomiting. Litoxetine has an affinity for brain 5HT3 receptors (Ki = 85 nM).

Tiflucarbine is a potential non-selective 5-HT agonist with antidepressant activity.Tiflucarbine dose-dependently increased the specific activity of soluble calmodulin (CaM)-dependent phosphodiesterase in rat brain.

p-MPPF dihydrochloride is a selective 5-HT antagonist that dose-dependently antagonizes hypothermia induced by 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and can be used to study neurological diseases.

p-MPPF is a selective 5-HT antagonist that dose-dependently antagonizes hypothermia induced by 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and can be used to study neurological diseases.

H1k is an eudistomin Y fluorescent derivative and lysosome-targeted antiproliferative agent that dose-dependently increases autophagy signalling and down-regulates the expression of cyclin-dependent kinase (CDK1) and cyclin B1.

USP28-IN-3 is a highly selective USP28 inhibitor with an IC50 value of 0.1 μM against USP28.USP28-IN-3 exhibits anticancer activity and inhibits USP2, USP7, USP8, USP9x, UCHL3, and UCHL5.USP28-IN-3 is cytotoxic to human colorectal and lung squamous carcinoma cells, inhibiting c-cells and c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-cells through the ubiquitin-proteasome system. -proteasome system to dose-dependently downregulate cellular levels of c-Myc.

Propane-1,2,3-triyl tripalmitate (Glycerol Tripalmitate) is a triacylglycerol found in dietary fats. In hamsters fed a diet enriched with it, Tripalmitin increases body weight, elevates plasma LDL levels, and reduces hepatic LDL receptor mRNA levels. It inhibits glucose-stimulated insulin secretion and decreases the viability of INS1 cells dose-dependently. Tripalmitin is used in cosmetic products for skin conditioning and as a thickening agent, and it forms lipid matrices of nanoparticles for drug delivery.

Galantide acetate, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide acetate recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide acetate dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide acetate appears to bind to a single population of SP receptors (KD~40 nM).

U-73343 is an inactive analog of U-73122 and can be used as a negative control. It dose-dependently inhibits acid secretion irrespective of the stimulant. It is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50 of 1-2.1 μM for PLC.

ELOVL6-IN-1 is a potent, orally active, and selective ELOVL6 inhibitor that dose-dependently inhibits mouse ELOVL6 activities with an IC50 value of 0.350 μM. It inhibits ELOVL6 in a noncompetitive manner for malonyl-CoA (Ki=994 nM) and palmitoyl-CoA[1].

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

PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC 50 of <40 nM for LOXL2 across all mammalian species and an IC 50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride dose-dependently reduced LOXL2-mediated collagen oxidation and collagen crosslinking in vitro which may represent an innovative therapeutic approach for the treatment of fibrosis

Aumitin, a diaminopyrimidine-based autophagy inhibitor, dose-dependently inhibits starvation- and rapamycin-induced autophagy with IC50s of 0.12 μM and 0.24 μM, respectively [1], and also inhibits mitochondrial respiration by targeting complex I.

CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins, dose-dependently inhibiting the TR-FRET signal between RGS4-AF488 and Tb-Gαo with an IC50 value of 1.9 μM.

PD 173212 is a blocker that blocks N-type voltage sensitive calcium channel (Cav2.2). PD173212 (0.0017-1.7 μmol/kg, Intraperitoneal Injection.) dose-dependently reduced DNBS-induced visceral hypersensitivity in mice.

PF-5006739 is a potent and selective CK1δ/ε inhibitor with IC50 values of 3.9 nM and 17.0 nM, respectively.It can be used in the study of psychiatric disorders and exhibits low nanomolar in vitro potency against CK1δ/ε and high kinome selectivity.PF-5006739 dose-dependently reduces opioid-seeking behavior in rodent relapse models and improves glucose tolerance in mouse models of diet-induced obesity (DIO) and genetic obesity (ob/ob).

sAJM589 is a Myc inhibitor that dose-dependently disrupts Myc-Max heterodimers, thereby decreasing Myc protein levels. Myc is a multifunctional nuclear phosphoprotein that plays a key role in cell cycle progression, apoptosis, and cellular transformation. sAJM589 inhibits the cellular proliferation of a variety of Myc-dependent cancer cell lines and the adherent, non-dependent growth of Raji cells’ Growth.