Nardosinonediol (Tetrahydronardosinon) is a serotonin transporter (SERT) inhibitor[1].
(4R)-2,2-Dimethyl-4-thiazolidinecarboxylic Acid is a cysteine derivative[1].
(-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca2+-permeable nonselective cation channel, to increase [Ca2+]i[1]. Antitumor activity[1].
W146 is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.
1,4-Diazabicyclo[2.2.2]octane-d12 is the deuterium labeled 1,4-Diazabicyclo[2.2.2]octane[1].
D-Alloisoleucine is an isoleucine derivative[1].
Chitinase-IN-2 is a insect chitinase and N- acetyl hexosaminidase inhibitor and pesticide; 50 μM/20 μM compound concentration's inhibitory percentage are 98%/92% for chitinase/N- acetyl-hexosaminidase respectively.
Guvacine, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively[1].
Megestrol Acetate is a synthetic progesteronal agent with an IC50 of 260 μM for the inhibition of HegG2.Target: Progesterone ReceptorMegestrol acetate, also known as 17α-acetoxy-6-dehydro-6-methylprogesterone, and sometimes abbreviated as MGA or MA, is a steroidal progestin and progesterone derivative (specifically, a 17-hydroxylated progesterone) with predominantly progestational and antigonadotropic effects. Megestrol acetate is a good candidate for muscle wasting treatment and future studies addressed at the interaction between the drug and protein turnover in human skeletal muscle should be performed.
Baccatin VI is a natural taxoid with antinociceptive activities. Baccatin VI possesses significant antinociceptive activity against p-Benzoquinone-induced abdominal contractions[1].
DY131(GSK 9089) is a novel selective agonist of ERRβ and ERRγ; displays minimal activity at ERRα, ERα and ERβ at concentrations up to 30 μM.IC50 value:Target: ERRβ/γDY131, a selective ERRγ agonist, could potentiate the ERRγ-induced growth inhibition in LNCaP- ERRγ and DU145- ERRγ cells in a dose-dependent manner compared with respective parental cells. DY131 inhibited the growth of the ERα-positive endometrial cancer cells but promoted that of the ERα-negative cancer cells. DY131 had no effect on the structurally related receptors ERRα or the estrogen receptors alpha and beta (ERalpha/beta). DY131 appears to inhibit Smo signaling through a common binding site shared by previously reported Smo agonists and antagonists.
Chikusetsusaponin Ib has anti-Alzheimer's disease activity and is a potent AChE inhibitor[1].
β,β-Dimethylacrylshikonin is a naphthoquinone derivative isolated from Arnebia nobilis, promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. Arnebin 1 has anti-tumor activity[1].
Hematoporphyrin dihydrochloride is a substrate for affinity chromatography of heme-binding proteins.Target: OthersHematoporphyrin is used for affinity chromatography of heme-binding proteins. Hematoporphyrin is used in the characterization and synthesis of hematoporphyrin- and hematin-agarose [1].
Metamitron is a pre- and post-emergence herbicide used for the control of broad-leaved weeds and grasses in sugar beet[1].
Vinpocetine(Cavinton; Ethyl apovincaminate) is a selective for PDE1 (IC50 = 21 μM). Also blocks voltage-gated Na+ channels.IC50 value:Target: PDE1; Na+ channel
Nattokinase is a potent fibrinolytic enzyme. Nattokinase can break down blood clots by directly hydrolyzing fibrin and plasmin substrate. Nattokinase can be used for the research of cardiovascular diseases[1].
mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM)[1].
Robinetin (3,3',4',5',7-Pentahydroxyflavone), a naturally occurring flavonoid with remarkable ‘two color’ intrinsic fluorescence properties, has antifungal, antiviral, antibacterial, antimutagenesis, and antioxidant activity. Robinetin also can inhibit lipid peroxidation and protein glycosylation[1][2][3][4][5].
Montelukast is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast can be used for the reseach of asthma and liver injury. Montelukast also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
ReAsH-EDT2 is a red fluorescent dye that marks proteins. ReAsH-EDT2 is a membrane-permeable biarsenical compound that binds covalently to tetracysteine sequences which allows the protein to be imaged. ReAsH-EDT2 can be used for protein localization and trafficking. (λex=530 nm, λem=592 nm)[1][2].
GGTI-2133 is a direct and selective inhibitor of geran ylgeranyltransferase (GGTase). GGTI-2133 has the potential for eosinophilic airway inflammation such as asthma research[1].
Jineol is a cytotoxic alkaloid from the centipede Scolopendra subspinipes. Jineol exhibits modest cytotoxic activity in vitro against the growth of human tumor cell lines[1].
Orcinol gentiobioside (compound 4) is a natural product isolated from the rhizomes of C. breviscapa[1].
KPT-8602 Z-isomer is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor.IC50：In Vitro: KPT 8602 Z-isomer exhibits different inhibitory effects on Z138, MM15, 3T3 cell lines, with IC50s of 100 nM-50 μM, < 100 nM, > 30 μM, respectively[1]. In Vivo:
Esperamicin A1, as an extremely potent antitumor antibiotic, is isolated from cultures of Actinomadura verrucosospora. Esperamicin A1 can be used for the research of antitumor[1].
H-Trp-Tyr-OH is adipeptide.
3-Hydroxy-7-methoxyflavone (compound 1) is a flavonoid. 3-Hydroxy-7-methoxyflavone is isolated from natural Salviaelegans. 3-Hydroxy-7-methoxyflavone has anti-anxiety effect[1].
GL189 is a β-secretase inhibitor. GL189 has neuroprotective effect, and can be used for research of neurodegenerative diseases[1].
Nafamostat hydrochloride, a synthetic serine protease inhibitor, is an anticoagulant.Target: Serine ProteaseTranilast (FUT-175) is an antiallergic drug for bronchial asthma. It has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis. It has also been investigated for use as an antiproliferative drug on drug-eluting stents.A 20-40 mg/h dose of FUT-175 prolonged coagulation time sufficiently in the instrumental blood of the extracorporeal circuit but not in the systemic blood. Its anticoagulant activity decreased immediately after hemodialysis. Therefore, we could manage all patients without any bleeding trouble during hemodialysis with FUT-175 as an anticoagulant. Although there were side effects of FUT-175, such as nausea, vomiting, itching and eruption, they were not serious, and FUT-175 could be administered without interruption. FUT-175 seems to be useful as an anticoagulant during hemodialysis for patients susceptible to bleeding.