Rafoxanide is a salicylanilide used as an antiparasitic agent.
SPV106 is histone acetylase (HAT) and GCN5-related N-acetyltransferases (GNAT) activator. SPV106 can be used for the research of type 2 diabetes (T2D)[1].
SEVNLDAEFR is a substrate for BACE1[1].
Isoxepac-d6 (HP 549-d6) is the deuterium labeled Isoxepac (HY-W050088). Isoxepac is a nonsteroidal anti-inflammatory agent[1].
Zilucoplan (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5 (C5) inhibitor. Zilucoplan can be used in research of immune-mediated necrotising myopathy (IMNM)[1][2].
(4Z)-Lachnophyllum lactone is a enyne derivative. (4Z)-Lachnophyllum lactone shows growth inhibitory activity against Lemna paucicostata (IC50=104 μM), which is a problematic and invasive weed[1].
VTP-27999 Hcl is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases.IC50 value:Target: Renin
Pimethixene is an antihistamine and anticholinergic agent, that is often used to treat hyperactivity, anxiety, sleep disorders, and allergy.
Kisspeptin 234, is a 10 amino acid peptide as well as a kisspeptin receptor (KISS1, GPR54) antagonist. Kisspeptin 234 is an analog of Kisspeptin 10[1].
Diazolidinyl urea, a broad spectrum preservative, is a formaldehyde-releasing compound that releases formaldehyde through its decomposition. Diazolidinyl urea is effective against most contaminating microorganisms, especially Pseudomonas[1][2].
SB 452533 is a potent and selective TRPV1 antagonist with the pKb of 7.8[1].
Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD)[1].
γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
Clonixin (SCH-10304) is an orally active analgesic and a non-steroidal anti-inflammatory agent in rodents[1].
Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors[1].
Oligomycin C is an antifungal agent isolated from Streptomyces strain[1].
Tiagabine hydrochloride(NO328 hydrochloride) is a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.Target: GABA reuptake inhibitorTiagabine had an early onset of effect, as shown by significant reduction from baseline in mean HAM-A total score compared with placebo at week 1 (observed cases, p < .05). Tiagabine was generally well tolerated and not associated with changes in sexual functioning or depressive status. Symptoms of a discontinuation syndrome during taper were not observed. Tiagabine may be a useful treatment option for adult patients diagnosed with GAD [1]. Tiagabine was generally well tolerated; the most common adverse events were nausea, dizziness and headaches [2]. Tiagabine (0.1 microM), an antiepileptic drug that specifically inhibits the GAT-1 GABA transporter inhibited GABA uptake 50% in temporal cortex and 60-68% in white structures [3].
Glutamate dehydrogenase NAD(P) (GLDH) can be found in hepatocytes, renal tissue, brain, muscle, and intestinal cells. Glutamate dehydrogenase NAD(P) is often used in biochemical studies. Glutamate dehydrogenase is a mitochondrial enzyme, it catalyzes the reversible oxidative deamination of glutamate to α-ketoglutarate (α-KG) as part of the urea cycle[1].
H-D-CHA-Ala-Arg-pNA is a chromogenic substrate for the amidolytic assay[1].
L-669,262, a potent inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, with an IC50 of 0.10 ng/mL for rat liver HMG-CoA[1].
PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases[1].
2,6-Dichloro-9-(2-c-methyl-2,3,5-tri-O-benzoyl-beta-D-ribofuranosyl)purine dibenzoate is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Acipimox is a niacin derivative used as a hypolipidemic agent.Target: Acipimox is a niacin derivative used as a hypolipidemic agent. It is used in low doses and may have less marked adverse effects, although it is unclear whether the recommended dose is as effective as are standard doses of nicotinic acid. Acipimox inhibits the production of triglycerides by the liver and the secretion of VLDL, which leads indirectly to a modest reduction in LDL and increase in HDL. Long-term administration is associated with reduced mortality, but unwanted effects limit its clinical use. Adverse effects include flushing (associated with Prostaglandin D2), palpitations, and GI disturbances. Flushing can be reduced by taking aspirin 20-30 min before taking Acipimox. High doses can cause disorders of liver function, impair glucose tolerance and precipitate gout. From Wikipedia.
SPL-334 is a potent and selective S-Nitrosoglutathione reductase (GSNOR) inhibitor. SPL-334 causes a significant reduction in the production of Th2 cytokines IL-5 and IL-13 and the levels of the chemokine CCL11 (eotaxin-1) in the airways. SPL-334 can be used in research of allergic airway inflammation[1].
o-3M3FBS is the negative control of m-3M3FBS. o-3M3FBS inhibits inward and outward currents via mechanisms independent of PLC acting in an antagonistic manner. In contrast, o-3M3FBS also causes an increase in [Ca2+]i in an agonistic manner[1].
Enoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects[1][2][3].
Isofebrifugine, isolated from a Chinese medicinal plant, Chang Shan (Dichroa febrifuga), is a natural quinazolinone alkaloid with important physiological activities and good pharmacological effects. Antimalarial effect[1].
LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors[1][2].
1-(2-Deoxy-β-D-threo-pentofuranosyl)thymine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
E3 Ligase Ligand-Linker Conjugates 25 Trifluoroacetate is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.