Others

Dihydroxy melphalan is an inactive degradation product of melphalan . It is formed by the hydrolysis of melphalan via the intermediate monohydroxy melphalan in aqueous solutions, including cell culture medium and human plasma.

DNP-INT is a quinone analog that inhibits electron transport in plants by competitively inhibiting plastoquinol oxidation by binding at the Qo site of cytochrome b6f (Kd = 1.4 nM). It inhibits electron flow from water to NADP or methylviologen by 50 and 100% when used at concentrations of 0.5 or 5 μM, respectively.

1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-PE is a phospholipid that contains stearic acid at the sn-1 position and 15(S)-HpETE at the sn-2 position. It is produced via oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-PE by 15-lipoxygenase (15-LO). 1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-PE (0.6 and 0.9 μM) increases ferroptotic cell death in wild-type and Acsl4 knockout Pfa1 mouse embryonic fibroblasts (MEFs) treated with the GPX4 inhibitor RSL3.

9-deoxy-9-methylene-16,16-dimethyl Prostaglandin E2 (Meteneprost) is a potent analog of prostaglandin E2 with an extended half-life in vivo. In combination with various other prostaglandin derivatives, it results in the termination of first trimester pregnancy in monkeys. A single intramuscular injection containing 0.5 mg of meteneprost and 7.5 mg of 17-phenyl trinor PGF1α is very effective in terminating early pregnancy. This prostaglandin mixture is ineffective on monkeys in their third trimester of pregnancy. Meteneprost, when compared to PGE2 and PGF1α, in monkey and rat, does not result in unwanted side effects such as fever or gastrointestinal problems.

6β-hydroxy Dexamethasone is a metabolite of dexamethasone that is more hydrophilic than the parent compound. Dexamethasone is metabolized by CYP3A4; therefore, quantification of the dexamethasone metabolites, 6α- and 6β-hydroxy dexamethasone, can be used to determine CYP3A4 enzyme activity in humans., The formation of 6-hydroxy dexamethasone metabolites is species-specific, with hamsters producing the highest amount. In rats, dexamethasone hydroxylation is sex-specific, with male rats producing metabolites in similar ratios to humans and female rats producing fewer hydroxylated metabolites than male rats.

Potent P2Y12 antagonist (IC50 = 17 nM). Displays antiplatelet and antithrombotic activity in vivo. Orally available. Boldron et al (2014) N-[6-(4-butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1H-indole-3-carboxamide (SAR216471), a novel intravenous and oral, reversible, and directly acting P2Y12 antagonist. J.Med.Chem. 57 7293 PMID:25075638

15(S)-HEDE is produced from 11Z,14Z-eicosadienoic acid by 15-LO. 15(S)-HEDE is an inhibitor of RBL-1 cell 5-LO with an IC50 value of 26 μM.

Dolutegravir M1 is a metabolite of the HIV integrase inhibitor dolutegravir .1It is formed primarily by the cytochrome P450 (CYP) isoforms CYP1A1 and CYP1B1. 1.Zhu, J., Wang, P., Li, F., et al.CYP1A1 and 1B1-mediated metabolic pathways of dolutegravir, an HIV integrase inhibitorBiochem. Pharmacol.158174-184(2018)

Mirtazapine N-oxide is a metabolite of mirtazapine.1It is formed from mirtazapine by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP3A4 in human liver microsomes.

(3S)-hydroxy Quinidine is an active quinidine metabolite. Quinidine, an antiarrhythmic agent, undergoes rapid first-pass metabolism by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C9, CYP2E1, and CYP3A5, with CYP3A4 being the most active enzyme in the (3S)-hydroxy quinidine formation. (3S)-hydroxy Quinidine prolongs repolarization of canine Purkinje fibers in vitro and prevents ventricular fibrillation and ventricular tachycardia after coronary reperfusion in isolated rat hearts in a dose-dependent manner.

Chlortetracycline is an analog of tetracycline , a broad spectrum antibiotic. In addition to its actions against microorganisms, chlortetracycline suppresses inflammation by inhibiting neutrophil action and other aspects of the innate immune response. 4-epi-Chlortetracycline is an epimer of chlortetracycline.

Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N/CD13 (IC50 = 25 μM). It is selective for AP-N/CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM.

5β-Dihydroprogesterone (5β-DHP) is a progesterone receptor agonist and metabolite of progesterone .1,2It is formed from progesterone by 5β-reductase.25β-DHP inhibits spontaneous contractions in isolated rat uterus when used at a concentration of 10 μg/ml, an effect that can be blocked by the progesterone receptor antagonist RU486 but not the GABAAreceptor antagonist picrotoxin .1It is a negative modulator of homooligomeric Ρ1 subunit-containing GABAAreceptors, inhibiting GABA-induced currents inX. laevisoocytes expressing these receptors (IC50= 5.02 μM).3Plasma levels of 5β-DHP decrease at the onset of spontaneous human labor.4

Ins(1,2)P2 (sodium salt) is one of the many inositol phosphate (InsP) isomers that could act as small, soluble second messengers in the transmission of cellular signals. The most studied InsP Ins(1,4,5)P3, is a second messenger produced in cells by phospholipase C (PLC)-mediated hydrolysis of phosphatidylinositol-4,5-biphosphate. Binding of Ins(1,4,5)P3 to its receptor on the endoplasmic reticulum results in opening of the calcium channels and an increase in intracellular calcium. Ins(1,2)P2 (tested as the D/L racemic mixture) is ~1,000-fold less potent than Ins(1,4,5)P3 at initiating Ca2+ release when injected into Xenopus oocytes.

Carbocyclic Thromboxane A2 可用于生命科学领域的相关研究。其产品编号为 T36548，CAS号为 74034-56-3。

(±)19(20)-EpDTE is an oxylipin and an oxidative metabolite of docosapentaenoic acid . It is formed via cytochrome P450 (CYP) metabolism of DPA and can be further metabolized to (±)19(20)-DiHDTE by epoxide hydrolase.

14,15-Leukotriene D4 (14,15-LTD4) is a member of an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-lipoxygenases (15- and 12-LOs) on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. 14,15-LTD4 is classified as an eoxin (EXD4), because it is formed mostly by eosinophils. However, mast cells and nasal polyps can synthesize 14,15-LTD4 as well. Little is known about the physiological actions of 14,15-LTD4. It has weak contractile activity on both guinea pig ileum and pulmonary parenchyma in contrast to the effects of 5-LO-derived LTs. However, in an in vitro permeability assay, 14,15-LTD4 can increase vascular permeability of human endothelial cell monolayers, with similar potency to that of 5-LO-derived LTs, resulting in plasma leakage, a hallmark of inflammation.

1-Oleoyl-2-palmitoyl-rac-glycerol (1,2-OP) is a diacylglycerol containing oleic acid at the sn-1 position and palmitic acid at the sn-2 position. It enhances the inhibition of superoxide anion production by cytochalasin B when used at a concentration of 10 μM. The concentration of 1,2-OP decreases from 25.7 to 11.15% during the dry-curing process of Iberian ham.

5(6)-EET is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5(6)-EET degrades into 5,6-DiHET and 5(6)-δ-lactone, which can be converted to 5(6)-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5(6)-EET has been implicated in the mobilization of calcium and hormone secretion. 5(6)-EET is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50 = 0.54 μM), and Cav3.3 and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5(6)-EET is provided as a mixture of the free acid and lactone.

(±)-PPCC 是 sigma-1 激动剂，能与 sigma-1 受体相互作用（Ki=1.5 nM）。(±)-PPCC 在有认知障碍的大鼠中具有抗遗忘作用，可以改善大鼠的认知能力。

Uridine-3'-monophosphate is a nucleoside used in the biochemical synthesis of ribothymidine-3'-phosphate. It has been used as a bioavailable source of uridine in research studies designed to enhance learning and memory.

Malformin C is a natural fungus-derived bicyclic pentapeptide that has antibacterial properties, particularly against species of Bacillus. Malformin C potently blocks the ability of bleomycin to induce G2 arrest in human T-cell leukemia-derived Jurkat cells (IC50 = 0.9 nM). It less potently abrogates colchicine-induced M phase arrest in Jurkat cells (IC50 = 24 nM). Malformin C inhibits cell growth dose-dependently in Colon 38 and HCT 115 cancer cells (IC50s = 0.27 and 0.18 μM, respectively) but has a low therapeutic index against cancer xenografts when tested in mice.

Nanatinostat, also known as Tractinostat, CHR-3996 and VRx-3996, is an orally bioavailable, second-generation hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor CHR-3996 inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes; these events may result in the inhibition of tumor cell division and the induction of tumor cell apoptosis. This agent may upregulate HSP70 and downregulate anti-apoptotic Bcl-2 proteins more substantially than some first-generation HDAC inhibitors. HDACs, upregulated in many tumor cell types, are a family of metalloenzymes responsible for the deacetylation of chromatin histone proteins.

Sezolamide is a carbonic anhydrase inhibitor.

Diclazuril K is a coccidiostat and GAPDH inhibitor used to prevent parasitic contamination of livestock and poultry feed.

Atiprimod is an orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.

SR-33805 is a calcium channel antagonist potentially for the treatment of atherosclerosis and heart failure. SR-33805 restored the MI-altered cell shortening without affecting the Ca(2+) transient amplitude, suggesting an increase of myofilament Ca(2+) sensitivity in MI myocytes. A SR33805-induced sensitization of myofilament activation was found to be associated with a slight increase in myosin light chain-2 phosphorylation and a more significant decrease on troponin I (TnI) phosphorylation. Decreased TnI phosphorylation was related to inhibition of protein kinase A activity by SR-33805.

Epetraborole is a potent and selective leucyl-tRNA synthetase inhibitor. Epetraborole was in development for the treatment of infections caused by multidrug-resistant Gram-negative pathogens.

Cenisertib benzoate is an orally bioavailable, synthetic, small-molecule multi-Aurora kinase inhibitor with potential antineoplastic activity.

Josamycin HCl is a macrolide antibiotic.

8-Azanebularine是通过将C6位的氨基替换为氢的化合物，能在高浓度(IC50=15 mM)下抑制ADAR2活性。该化合物在人类ADAR2识别的RNA结构中插入，展示出高亲和力(KD=2 nM)。因此，8-Azanebularine可应用于研究ADAR催化的RNA编辑过程。

Glasdegib hydrochloride is a small-molecule inhibitor of the Hedgehog (Hh) signaling pathway with potential antineoplastic activity.

Migalastat (GR181413A free base) 是一种具有口服活性和竞争性的α-galactosidase A 抑制剂，对人α-Gal A 的IC50值为 0.04 μM。

BEPP monohydrochloride is a double-strand RNA-dependent protein kinase (PKR) activator.

9-(Boc-amino)nonanoic Acid is an alkane chain with terminal carboxlic acid and Boc-protected amino groups. The compound can be used as a PROTAC linker in the synthesis of PROTACs. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond. The Boc group can be deprotected under mild acidic conditions to form the free amine.

N-Fmoc-8-aminooctanoic acid can be used as a PROTAC linker in the synthesis of PROTACs. N-Fmoc-8-aminooctanoic acid is an alkane chian with terminal Fmoc-protected amine and carboxylic acid groups. The Fmoc group can be deprotected under basic condition to obtain the free amine which can be used for further conjugations. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond.