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].
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].
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].
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.
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].
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].
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.
7-O-Methylbiochanin A (4',7-Dimethoxy-5-hydroxyisoflavone) is an isoflavone derivative isolated from the roots of Lotus polyphyllos[1].
OV-1, sheep is an alpha-helical antimicrobial ovispirin peptide derived from SMAP29 peptide (sheep), which inhibits several antibiotic-resistant bacterial strains including mucoid and nonmucoid Pseudomonas aeruginosa[1].
Hemin is an iron-containing porphyrin. Hemin is an Heme oxygenase (HO)-1 inducer.
Valomaciclovir stearate (ABT 606), a nucleoside analog, is the Omaciclovir (HY-116174) prodrug. Valomaciclovir stearate has antiviral activity against HSV-1 and varicella zoster virus (VZV)[1].
Sodium methanesulfonate-d3 is the deuterium labeled Sodium methanesulfonate[1].
VX-702 is a highly selective inhibitor of p38α MAPK(IC50=4 -20 nM), 14-fold higher potency against the p38α versus p38β.IC50 value: 4-20 nM [1]Target: p38α MAPKin vitro: Pre-incubation of platelets with VX-702 (1 μM) completely or partially inhibits p38 activation (IC50 4 to 20 nM) induced by platelet agonists including thrombin, SFLLRN, AYPGKF, U46619 and collagen. VX-702 shows no effect on platelet aggregation induced by any of the p38 MAPK agonists in the presence or absence of anti-platelet therapies [1]. VX-702 inhibits the production of IL-6, IL-1β and TNFα (IC50 = 59, 122 and 99 ng/mL, respectively) in a dose-dependent manner [2]. in vivo: The half-life of VX-702 is 16 to 20 hours, with a median clearance of 3.75 L/h and a volume of distribution of 73 L/kg. Both AUC and Cmax values are dose proportional for VX-702, which is predominantly cleared renally [2]. VX-702 (at a dose of 0.1 mg/kg twice daily) has an equivalent effect as that of methotrexate (0.1 mg/kg). In addition, VX-702 (5 mg/kg twice daily) also has an equivalent effect as prednisolone (10 mg/kg once daily), as measured by percentage inhibition of wrist joint erosion and inflammation score [3].
S-(4-Hydroxybenzyl)glutathione is a glutathione derivative. S-(4-Hydroxybenzyl)glutathione inhibits the in vitro binding of kainic acid to brain glutamate receptors, with an IC50 of 2 μM[1].
Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, hypnotic, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K⁺ channel pathway[1][2].
(R)-2-Hydroxysuccinic acid methyl ester is a biochemical that can be used for the research of cancer or amyloidosis[1].
True Blue (NCI 240899) is a fluorescent dye, as neuronal retrograde tracer (excitation wavelength 395-425 nm, barrier filter 450 nm). True Blue can label neuron and has no effects on neuronal survival[1][2].
PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively[1].