Compound cpd-1 is a small molecule Trks inhibitor with good antitumor activity[1].
Quinovic acid 3-O-β-D-quinovopyranoside is a tritenpenoid glycoside, that can be isolated from the bark of L. hexandra[1].
Quinocetone is a potent synthetic antimicrobial agent that is used for improving the feed efficiency and controlling dysentery in food-producing animals[1].
BMS-919373 is a selective, potent IKur current blocker. BMS-919373 can be used for the research of cardiovascular diseases[1].
Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.
Dimethylfraxetin is a Carbonic anhydrase inhibitor, with a Ki value of 0.0097 μM.
DMT-dG(ib) Phosphoramidite-13C10,15N5 is the 13C and 15N labeled DMT-dG(ib) Phosphoramidite[1]. DMT-dG(ib) Phosphoramidite is typically used in the synthesis of DNA[2].
D-Arg-[Hyp3,Thi5,8,D-Phe7]-Bradykinin is a biological active peptide. (inhibited bradykinin-induced contractions concentration dependently; bradykinin B2 receptor antagonist)
Dihydrolycorine is isolated from Lycoris radiate Herb with antihypertensive and neuroprotective activities[1]. Dihydrolycorine is an inhibitor of protein synthesis in eukarytic cells by inhibiting the peptide bone formation step[2].
Sibiricose A6 is an oligosaccharide ester isolated from Polygalae Radix with potent antioxidant activity[1][2].
Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders.
R-IMPP is an inhibitor of PCSK9 secretion.
3’-beta-Azido-2’,3’-dideoxy-5’-O-(4-methoxy-trityl)uridine 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].
α-Conotoxin EI is a selective nicotinic acetylcholine α1β1γδ receptor (nAChR) antagonist (IC50=187 nM) and an α3β4 receptor inhibitor. α-Conotoxin EI can block muscle and ganglionic receptors[1][2][3].
TKIM is a TREK-1 channel inhibitor with an IC50 of 2.96 μM. TKIM binds to the pocket of the intermediate (IM) state of TREK-1[1].
Abz-AGLA-Nba is a fluorogenic substrate for the determination of protease activity. Abz-AGLA-Nba is hydrolyzed to release aminoacyl benzimide (Abz-AGLA) and 2-naphthylaminoacyl (Nba). The product Abz-AGLA produced by this hydrolysis reaction is fluorescent under ultraviolet light and can emit a fluorescent signal[1].
2,2-Dibromopropanoic acid is a dibromo product based on panoic acid. Propionic acid is a short chain fatty acid and acts as chemical intermediate. Propionic acid is also a mold inhibitor and widely used in food preservative[1].
Quinapril is a prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications.Target: ACEQuinapril is an angiotensin-converting enzyme inhibitor (ACE inhibitor) used in the treatment of hypertension and congestive heart failure. Quinapril is rapidly de-esterified after absorption to quinaprilat (the active diacid metabolite), a potent angiotensin converting enzyme (ACE) inhibitor. Quinapril is now firmly established as an effective and well tolerated ACE inhibitor for the treatment of patients with hypertension and congestive heart failure. Quinapril 40 mg/day also significantly reduced the incidence of ischaemic events in patients undergoing CABG in one study [1, 2]. An overview of 32 clinical trials of ACE inhibitors in heart failure showed that no significant heterogeneity in mortality was found among enalapril, ramipril, quinapril, captopril, lisinopril, benazepril, perindopril and cilazapril. Initiation of therapy with captopril, ramipril, and trandolapril at least 3 days after an acute MI resulted in all-cause mortality risk reductions of 18 to 27% [3].
Axitinib analogue 1 is a analogue of Axitinib (HY-10065).
Sphondin, isolated from Heracleum laciniatum, possesses an inhibitory effect on IL-1β-induced increase in the level of COX-2 protein and PGE2 release in A549 cells[1].
Tenatoprazole (TU-199) is an orally active imidazopyridine-based proton pump inhibitor with a prolonged plasma half-life. Tenatoprazole inhibits hog gastric H+/K+-ATPase activity with an IC50 of 6.2 μM. Tenatoprazole blocks the interaction of ubiquitin with the ESCRT-1 factor Tsg101, inhibits production of several enveloped viruses, including EBV[1][2][3].
Ceanothic acid (Emmolic acid) is a ring-A homologue of betulinic acid. Ceanothic acid inhibits OVCAR-3, HeLa, and FS-5 cells with the cell survival of 68%, 65%, and 81%, respectively[1].
(Des-Gly10,D-Leu6,Orn8,Pro-NHEt9)-LHRH is a biologically active peptide.
Spisulosine-d3 is deuterium labeled Spisulosine. Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKC
N-Methyl-N-[4-(methylthio)-1,3-benzothiazol-2-yl]glycine is a Glycine (HY-Y0966) derivative[1].
Sulfazamet-13C6 is the 13C6 labeled Sulfazamet.
Nε-Acetyl-L-lysine (hydrochloride) is a peptide derivatives, shows antiviral activity[1].
Obexelimab (XmAb5871) is a humanized anti-CD19 antibody Fc-engineered for increased affinity to FcγRIIb. Obexelimab can be used in research of autoimmune[1].
Coprelotamab (GB-221) is an IgG-κ monoclonal antibody targeting EGFR2. The commonly used expression system for Coprelotamab is CHO DG44 (Chinese Hamster Ovary) cells[1].
AVN-944(VX-944) is a selective, noncompetitive inhibitor of the enzyme directed against human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2.IC50 value: 6-10 nM (Ki) [1]Target: IMPDHin vitro: AVN-944 strikingly inhibit RNA synthesis within 2 h of exposure. Depletion of guanine nucleotides by MPA and AVN-944 also causes an early and near-complete reduction in levels of the 45S precursor rRNA synthesis and the concomitant translocation of nucleolar proteins including nucleolin, nucleophosmin, and nucleostemin from the nucleolus to the nucleoplasm [2]. AVN944 induced caspase-dependentand caspase-independent cell death in LNCaP, CWR22Rv1, and DU145 cells. AVN944 induced expression of p53-target proteins Bok, Bax and Noxa in androgen-responsive cell lines and suppressed expression of survivin in prostate cancer cells regardless of their androgen sensitivity. AVN944 also induced differentiation of androgen-independent prostate cancer cells as indicated by morphological changes and increased expression of genes coding for prostasomal proteins, keratins and other proteins, including tumor suppressor genes MIG-6 and NDRG1. AVN944-differentiated androgen-independent DU145 and PC-3 cells are sensitized to TRAIL-induced apoptosis as demonstrated by induction of caspases and PARP cleavage [3].