Bakuchiol is a phytoestrogen isolated from the seeds of Psoralea corylifolia L; has anti-tumor effects.IC50 value:Target:in vitro: Bakuchiol reduced mitochondrial membrane potential (Psim) of cells in a concentration- and time-dependent manner, showing a more potent effect than that of resveratrol. S phase arrest, caspase 9/3 activaton, p53 and Bax up-regulation, as well as Bcl-2 down-regulation were observed in bakuchiol-treated A549 cells [1]. UGT2B7 was inhibited by the strongest intensity. The noncompetitive inhibition was demonstrated by the results obtained from Dixon plot and Lineweaver-Burk plot. The Ki value was calculated to be 10.7 μM [2]. Bakuchiol was found to be naturally occurring potent inhibitors of hCE2, with low Ki values ranging from 0.62μM to 3.89μM [3]. After exposure to bakuchiol at 0.25-fold, 0.5-fold and 1-fold of minimum inhibitory concentration (MIC) (3.91 μg/ml) for 24h, the fungal conidia of T. mentagrophytes demonstrated a significant dose-dependent increase in membrane permeability. Moreover, bakuchiol at 1-fold MIC elicited a 187% elevation in reactive oxygen species (ROS) level in fungal cells after a 3-h incubation [4].in vivo: In combination with the reported concentration after an intravenous administration of bakuchiol (15 mg/kg) in rats, the high risk of in vivo inhibition of bakuchiol towards UGT2B7-catalyzed metabolism of drugs was indicated [2]. In a guinea pig model of tinea pedis, bakuchiol at 1%, 5% or 10% (w/w) concentration in aqueous cream could significantly reduce the fungal burden of infected feet (p<0.01-0.05) [4].
Ajugalide D, a neoclerodane diterpene, is nature product that could be isolated from Ajuga taiwanensis[1].
L-Lysyl-L-lysine (Lysyllysine) dihydrochloride is an enzyme cleavable basic amino acid. L-Lysyl-L-lysine dihydrochloride can be used for delivering multiple biologically active peptides[1].
Ghrelin receptor full agonist-2 is a highly potent Ghrelin receptor full agonist.
Huzhangoside C is a oleanane-type triterpenoid saponin that can be isolated from the roots of Clematis argentilucida[1].
Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC50 of 29 nM.
8(14)-Abietenic acid is an abietane diterpenoid. Abietenic acid is racemic of 8(14)-Abietenic acid. Abietenic acid acts as a PPARα/γ dual activator[1][2].
(S)-Lisofylline ((S)-Lisophylline)) is a kind of lisofline (LSF) enantiomer with optical activity. (S)-Lisofylline can interconversion with pentoxifylline[1][2].
DBPR112 (compound 78) is an orally active Furanopyrimidine-Based Epidermal Growth Factor Receptor inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. DBPR112 has significant antitumor efficacy[1].
(Rac)-ICI-118551 hydrochloride is a selective β2-adrenergic receptor antagonist. (Rac)-ICI-118551 hydrochloride can inhibit dendrite ramification of hippocampal neurons in a mouse model of Alzheimer's disease[1].
Nogalamycin is an anthracyclinone antibiotic. Nogalamycin is a potent antibiotic against Gram-positive bacteria, also has cytotoxicity against certain tumor cells. Nogalamycin is produced by Streptomyces nogalater var. Nogalater. Nogalamycin selectively inhibits RNA synthesis after binding to DNA template. Nogalamycin can be used for researching anticancer[1][2].
Kaempferol-3-O-(6′′-galloyl)-β-glucopyranoside is a glucopyranoside. Kaempferol-3-O-(6′′-galloyl)-β-glucopyranoside inhibts HIV-2 RNase H with an IC50 value of 5.19 μM[1].
TP-051 is a potent FFAR1 agonist with an Ki value of 16 nM for human FFAR1. TP-051 can increase insulin secretion in rat insulinoma cells. TP-051 can be used to research type 2 diabetes[1].
Physapruin A is a withanolide that can be found in Physalis pruinosa[1].
NSC363998 (free base) is an orally active compound. NSC363998 (free base) can suppress rCGG90 induced neurotoxicity. NSC363998 (free base) can be used for the research of neurodegenerative disorder such as Fragile X associated tremor/ataxia syndrome (FXTAS)[1].
3,4,5-Trimethoxyphenyl-(6' -o-galloyl) -o-β-d-Glucopyranoside is a phenylpropanoside derived from natural the bark of Streblus ilicifolius (Vidal)[1].
(D-Trp6)-LHRH-Leu-Arg-Pro-Gly amide is a biologically active peptide.
Alloferon 2 is an antiviral and antitumoral peptide. Alloferon 2 can be isolated from the blood of the blow fly Calliphora vicina (Diptera)[1].
PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I (PAC1) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain[1].
E 2012 is a potent γ-secretase modulator.IC50 value:Target: γ-secretaseIn the present study, 9 dogs were treated with a single dose of the γ-secretase modulator E2012, the γ-secretase inhibitor LY450139, or vehicle with a dosing interval of 1 week. The isoform Aβ(1-37) was significantly increased in a dose-dependent manner in response to treatment with E2012, while Aβ(1-39), Aβ(1-40) and A(1-42) decreased [1].E2012, a gamma secretase modulator without affecting Notch processing, aimed at Alzheimer's disease by reduction of amyloid β-42, induced cataract following repeated doses in the rat.E2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. In vivo lenticular concentration of E2012 after 13-week repeated dose with cataract was well above those where inhibition was observed in vitro.E2012 induces cataract in the rat by inhibiting DHCR24 at the final step of cholesterol synthesis with associated elevation in desmosterol within the lens, preceded by desmosterol changes that would serve as a predictive safety biomarker for lenticular opacity [2].
Benzalkonium chloride is a potent anti-microbial agent, used as a preservative in eye drops.
Iprobenfos is an organophosphorus fungicide and is widely used to control the rice blast fungus. Iprobenfos is also a choline biosynthesis inhibitor[1][2].
[D-Trp8] Somatostatin-14, a tetradecapeptide, is an analog of Somatostatin more potent than the native Somatostatin[1].
Bromhexine Hydrochloride is a medication prescribed for coughs which works by dissolving hard phlegm.Target: OthersBromhexine is a mucolytic agent used in the treatment of respiratory disorders associated with viscid or excessive mucus. In addition, bromhexine has antioxidant properties. Bromhexine is intended to support the body's mechanisms for clearing mucus from the respiratory tract. Bromhexine is a synthetic derivative of the herbal active ingredient vasicine. It has been shown to increase the proportion of serous bronchial secretion, making it more easily expectorated. It is indicated as "secretolytic therapy in bronchopulmonary diseases associated with abnormal mucus secretion and impaired mucus transport". From Wikipedia. [1]
Albanol B is an arylbenzofuran derivative which can be isolated from mulberries. Albanol B exhibits anti-Alzheimer's disease, anti-bacterial and antioxidant activities. Albanol B inhibits cancer cells proliferation, down-regulates CDK1 expression. Albanol B also induces cell cycle arrest at G2/M and apoptosis. And Albanol B induces mitochondrial ROS production and increases the phosphorylation levels of AKT and ERK1/2[1].
CL2A is a complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. Labetuzumab govitecan used this linker[1].
DMT-2'-F-Bz-dA can be used in the synthesis of nucleotides and nucleic acids.
Phytochelatin 6 is metal-binding compound produced by plants. Phytochelatin 6 may reduce bioavailability of dietary toxic metals such as cadmium[1].
Sparfloxacin is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity.Target: AntibacterialSparfloxacin shows broad and potent antibacterial activity. Its MICs for 90% of the strains tested are 0.1 to 0.78 μg/ml against gram-positive organisms, such as members of the genera Staphylococcus , Streptococcus and Enterococcus , and 0.0125 to 1.56 μg/ml against gram-negative organisms, such as members of the family Enterobacteriaceae and the genera Pseudomona . Its MICs are 0.025 to 0.78 μg/ml against glucose nonfermenters, 0.2 to 0.78 μg/ml against anaerobes, 0.0125 to 0.05 μg/ml against Legionella. Sparfloxacin showed good oral efficacy against systemic infections with Staphylococcus aureus , Streptococcus pyogenes , Streptococcus pneumoniae , Escherichia coli , and Pseudomonas aeruginosa in mice [1]. Sparfloxacin targets DNA gyrase and inhibits DNA synthesis [2].
Bimosiamose is a pan-selectin antagonist, inhibits E-, P-, and L-selectin with IC50s of 88 μM, 20 μM, and 86 μM, respectively, and can be used in the research of inflammatory disease.