8α-Tigloyloxyhirsutinolide 13-O-acetate is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and Pyroptosis, and late DNA damage, cell cycle arrest, Apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo[1][2].
Levophacetoperane inhibits in vitro in a competitive manner, norepinephrin uptake and dopamine uptake.
ω-Conotoxin GVIA is an inhibitor of the N-type Ca2+ channel[1].
CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.
BMS 753 is an isotype-selective retinoic acid receptor α (RARα) agonist, with a Ki of 2 nM[1].
CM121 is an active site-directed reversible ALDH1A2 inhibitor (IC50=0.54 μM；Kd=1.1 μM) with a variety of hydrophobic interactions[1].
Acetyl-α-MSH (11-13) is the acetylated C-terminal tripeptide of α-MSH with antipyretic and anti-inflammatory activities[1][2].
MMAF hydrochloride is an antitubulin agent that inhibit cell division; inhibits H3397 cell growth with an IC50 of 105 nM.
BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM.
DDO-02005 is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine[1].
Methyl kakuol shows agonistic activity against TRPA1 with an EC50 of 0.27 µM[1].
Roflumilast Impurity E is the impurity of Roflumilast. Roflumilast(Daliresp) is a drug which acts as a selective and long-acting inhibitor of the enzyme PDE-4 with an IC50 value of 0.8 nM.
Tetanus Toxin (830–844) is a biological active peptide. (tetanus toxin-derived peptide TT830–844 CD4+ T-cell epitope. This promiscuous CD4+ T-cell epitope can bind to a wide range of HLA–DRB molecules and is thus expected to activate CD4+ T-cell responses in a large part of the human population)
Dinotefuran is an insecticide of the neonicotinoid class, its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors.Target: nAChR, Antiparasitic
Parstatin(mouse), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis[1][2].
GAL-021 a new intravenous BKCa-channel blocker.
10-10-Hydroxyaloin A is potent SARS-CoV-2 inhibitor. 10-Hydroxyaloin A exhibits significant efficacy to bind SARS-Cov-2 Mpro active site[1].
EPZ011989 trifluoroacetate is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.IC50 value: < 3 nM ( Ki for wt EZH2, EZH2 Y646)Target: EZH2 inhibitorIn vitro: EPZ011989 is also a specific EZH2 inhibitor with a >15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. EPZ011989 also exhibits metabolic stability. Furthermore, EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. This functional response translates to activity in a long-term proliferation assay where EPZ011989 demonstrates an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM. In vivo: The LCC parameter, when corrected for plasma protein-binding, predicts an efficacious plasma level in mouse for EPZ011989 of 158 ng/mL. The pharmacokinetics in SCID mice following oral administration of 125, 250, 500, and 1000 mg/kg indicated that the 1000 mg/kg dose provided coverage over the LCC for 24 h, while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.
Alisol B 23-acetate, a natural triterpenoid, produces protective effects against EE-induced cholestasis, due to FXR-mediated gene regulation.IC50 Value:Target: Anti-hepatotoxic natural product. In vitro: Alisol-B 23-acetate has an effect on FXR activation in a dose-dependent manner using luciferase reporter assay in HepG2 cells [3].In vivo: In alisol B 23-acetate-treated mice, the changes in transporters and enzymes, as well as ameliorative liver histology were abrogated by FXR antagonist guggulsterone [1]. Alisol B 23-acetate treatment in a dose-dependent manner resulted in protection against hepatotoxicity induced by CCl4via FXR activation. Through FXR activation, alisol B 23-acetate promoted hepatocyte proliferation via an induction in hepatic levels of FoxM1b, Cyclin D1 and Cyclin B1. Alisol B 23-acetate also reduced hepatic bile acids through a decrease in hepatic uptake transporter Ntcp, bile acid synthetic enzymes Cyp7a1, Cyp8b1, and an increase in efflux transporter Bsep, Mrp2 expression. In addition, alisol B 23-acetate induced the expression of STAT3 phosphorylation, and STAT3 target genes Bcl-xl and SOCS3, resulting in decreased hepatocyte apoptosis [2].
Chromocarb is a synthetic vasoprotectant.
(S)-(-)-HA 966 ((-)-HA 966), a γ-Hydroxybutyrate-like agent, is weakly active as an NMDA-receptor antagonist. (S)-(-)-HA 966 possesses muscle relaxant action and prevents enhanced mesocorticolimbic dopamine metabolism and behavioral correlates of restraint stress, conditioned fear[1][2].
Naltriben mesylate is a potent delta-2 receptor-selective antagonist, with Kis are 0.013, 19 and 152 nM for δ, μ and κ receptors respectively. Naltriben mesylate selectively attenuates alcohol intake in rats bred for alcohol preference[1][2].
(R)-2-((S)-2-amino-4-methylpentanamido)-4-methylpentanoic acid dihydrate is a leucine derivative[1].
Agalsidase alfa has an amino acid sequence identical to that of native α-galactosidase A. Agalsidase alfa can be used for Fabry disease research[1].
Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a Kd of 5 nM, shows effective anti-HCV activity, with an EC50 of 98 nM for HCV 2a[1].
Influenza A NP(366-374) Strain A/PR/8/35 is an H2-Db-restricted epitope from Influenza A/PR/8/35 nucleoprotein[1].
MPX-004 is a potent GluN2A antagonist. MPX-004 inhibits GluN2A-containing NMDA receptors expressed in HEK cells with an IC50 of 79 nM. MPX-004 has no inhibitory effect on GluN2B or GluN2D receptor-mediated responses. MPX-004 has the potential for neuropsychiatric and developmental disorders research[1].
Cyanine3 amine hydrochloride, an analog of Cyanine3 amine, is a potent green fluorescent dye. Cyanine3 amine hydrochloride has the primary amine group and is covalently coupled with reactive groups such as NHS esters, carboxy groups (after carbodiimide activation), and epoxides. (λex=555 nm, λem=570 nm)[1].
Succinic anhydride is a cyclic anhydride and an ADC linker extracted from patent WO2009064913A1. It can react with compound 4 of the patent to link the prodrug to an amine or hydroxy 1 group of a targeting polypeptide[1].
Fadrozole hydrochloride hemihydrate is an orally active, potent, selective and nonsteroidal aromatase inhibitor, with an IC50 of 6.4 nM. Fadrozole hydrochloride hemihydrate inhibits the production of estrogen and progesterone, with IC50 values of 0.03 and 120 μM. Fadrozole hydrochloride hemihydrate shows prevention of spontaneous tumours. Fadrozole hydrochloride hemihydrate can be used for the research of estrogen-dependent disease and cancer[1][2][3].