sam

SAM-315 (WAY-255315) is a potent antagonist of 5-Hydroxytryptamine-6 (5-HT6), with Ki and IC50 values of 1.1 nM and 4.6 nM, respectively. SAM-315 notably enhances the release of acetylcholine and glutamate in the hippocampus of the brain.

AG-270 is an allosteric and orally active inhibitor of MAT2A.

FIDAS-3, a stilbene derivative and potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A), exhibits anticancer activities by effectively competing with S-adenosylmethionine (SAM) for MAT2A binding.

FIDAS-5 is an orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. It can effectively compete with S-adenosylmethionine for MAT2A binding and has anticancer effects.

Cerlapirdine (PF-05212365) is a selective, potent, full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine is already in clinical development for the treatment of cognitive disorders related to Alzheimer's disease and schizophrenia. It works by acting as a selective 5-HT6 receptor antagonist.

Cerlapirdine, also known as SAM-531, WAY-262,531 and PF-05212365, is a selective, potent, full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has been in clinical development for the treatment of cognitive disorders associated with Alzheimer's disease and schizophrenia. As of 2011, it is in phase II clinical trials, and has demonstrated a trend toward efficacy along with a good side effect profile and no incidence of serious adverse events. It exerts its effects by acting as a selective 5-HT6 receptor antagonist.

MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. MHY219 effectively increased the sub-G1 fraction of cells through p21 and p27 dependent pathways in DU145 cells. MHY219 significantly induced a G2/M phase arrest in DU145 and PC3 cells and arrested the cell cycle at G0/G1 phase in LNCaP cells. Furthermore, MHY219 effectively increased apoptosis in DU145 and LNCaP cells, but not PC3 cells, according to Annexin V/PI staining and Western blot analysis. These results indicate that MHY219 is a potent HDAC inhibitor that targets regulating mu......

Sardomozide is an inhibitor of S-adenosylmethionine decarboxylase (SAMDC)(IC50 of 5 nM).

S-adenosylmethionine is a precursor of taurine and cysteine, acting through methylation, sulphuration, and peptide synthesis. It promotes the formation of the MetJ-DNA complex, a transcription repressor of methionine in E. coli.

PF-05212377 (SAM-760) is an inhibitor of the serotonin receptor 5-HT6. It acts as a substrate for the human transport proteins P-gp/non-BCRP. The compound has demonstrated blood-brain barrier permeability in non-human primates. PF-05212377 is utilized in research related to Alzheimers disease.

Dp3-Sam chloride (Standard) is a reference standard for research and analysis in studies involving Dp3-Sam chloride. Dp3-Sam chloride (Delphinidin-3-sambubioside chloride) is an anthocyanin from Hibiscus acetosella (Cranberry Hibiscus) with anti-inflammatory, antioxidant, and anticancer activities.Dp3-Sam chloride inhibits LPS-induced inflammation, and inhibits LPS-induced inflammation. Dp3-Sam chloride inhibits LPS-induced inflammatory factor release, down-regulates the NF-κB pathway, and inhibits MEK1/2-ERK1/2 signaling.Dp3-Sam chloride induces apoptosis in human leukemia cells through the mitochondrial pathway mediated by reactive oxygen species.

Dp3-Sam chloride (Delphinidin-3-sambubioside chloride) is an anthocyanin from Hibiscus acetosella (Cranberry Hibiscus) with anti-inflammatory, antioxidant, and anticancer activities.Dp3-Sam chloride inhibits LPS-induced inflammation, and inhibits LPS-induced inflammation. Dp3-Sam chloride inhibits LPS-induced inflammatory factor release, down-regulates the NF-κB pathway, and inhibits MEK1/2-ERK1/2 signaling.Dp3-Sam chloride induces apoptosis in human leukemia cells through the mitochondrial pathway mediated by reactive oxygen species.

SAMβA TFA, a selective antagonist of Mfn1-βIIPKC association conjugated to the cell permeable peptide TAT47-57, is a rationally designed inhibitor that improves heart failure outcomes in rats [1].

TAT-SAMβA, an RNAENFDRF (SAMβA) peptide conjugated to the TAT 47–57 protein-derived cell-penetrating peptide, acts as a selective antagonist of the Mfn1-βIIPKC association. It has been shown to protect mouse embryonic fibroblast cells (MEFs) from cytotoxicity induced by oxidative stress [1].

4-Methyl-2-oxopentanoic acid is an abnormal metabolite, a neurotoxin and a metabolic toxin.

Niclosamide (Niclocide)(BAY2353) is used to treat most tapeworm infections by inhibiting DNA replication.

Adhesamine, a dumbbell-shaped molecule, plays a crucial role in activating the MAPK/FAK pathway, thus promoting mammalian cell adhesion and growth. Additionally, it accelerates the differentiation and enhances the survival of mice hippocampal neurons in primary culture.

Sesamodil (SD 3211) is a novel calcium antagonist that can be used to study hypertension.

Iso-Samidorphan is a biochemical reagent that can be used in biological experiments.

Samidorphan HCl is an orally active and highly potent modulator of the opioid system that binds to μ‐opioid, κ‐opioid, and delta-opioid receptors. Samidorphan HCl is a novel μ-opioid receptor antagonist, a partial agonist for k-opioid and delta-opioid receptors. Samidorphan HCl can be used to prevent and treat schizophrenia.

(Iso)-Samixogrel shows activity against Carbonic anhydrase and Cyclooxygenase 2.

Amakusamine is an indole alkaloid from the sponge of Psammocinia sp. It inhibits RANKL-induced isolation of multinucleated osteoclasts and inhibits RANKL-induced multinucleated osteoclasts.

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.

Glucosamine (Chitosamine) is a natural product. Glucosamine is used as a dietary supplement. Glucosamine has pharmacological effects on cartilage and chondrocytes in osteoarthritis when used externally. Glucosamine regulates sugar metabolism. Glucosamine reduces the activity of glucoskinase in pancreatic islet homogenate.