Stemonidine is a natural Stemona alkaloid[1].
Malathion is an organophosphate parasympathomimetic which binds irreversibly to cholinesterase, is an insecticide of relatively low human toxicity.
RPR104632 is a specific antagonist of NMDA receptor, with potent neuroprotective properties.
STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively.
XE 991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC50s of 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively[1].
Deruxtecan-d4-1 is the deuterium labeled Adenosine 5'-monophosphate disodium salt[1].
Benzyl-PEG2-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Belrestotug (EOS-448) is an antagonistic anti-TIGIT (VSIG9, VSTM3) human immunoglobulin G1 kappa (hIgG1 kappa) antibody. Belrestotug shows antineoplastic activity[1].
Cap-dependent endonuclease-IN-19 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-19 is a spirocyclic pyridone derivative. Cap-dependent endonuclease-IN-19 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent CN111410661A, compound 1)[1].
Dansyl-Ala-Arg is a synthetic peptide. Dansyl-Ala-Arg can be used for various biochemical studies[1].
TCO-PEG3-maleimide (TCO-PEG3-NEM) is a click chemistry reagent. TCO-PEG3-maleimide efficiently binds TCO (trans-cyclooctene) moiety to thiol-containing molecules (such as antibodies, cysteine-containing peptides)[1].
MELK-8a (NVS-MELK8a) is a highly potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor with IC50 of 2 nM. MELK-8a also inhibits Flt3 (ITD), Haspin, PDGFRα with IC50s of 0.18, 0.19, and 0.42 μM, respectively. MELK plays an essential role in regulating cell mitosis in a subset of cancer cells[1].
Cockroach Myoactive Peptide I (Pea-CAH-I) is a cockroach neuropeptide, a member of the adipokinetic hormone/red pigment-concentrating hormone family (AKH/RPCH family)[1].
Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent.
Influenza virus NP (266-274) is a biological active peptide. (HLA-A*03 restricted epitope from influenza virus nucleoprotein (265-274).)
m-PEG4-SH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Tamoxifen is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.
3-Deaza-4’-C-methyluridine, 4-Hydroxy-1-β-D-(4-C-methylribofuranosyl)-2(1H)-pyridinone is a purine nucleoside analogue. 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].
Tetrahydrocurcumin is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin inhibit CYP2C9 and CYP3A4.
D-Lactate dehydrogenase (D-LDH) is an oxidoreductase that uses NAD+ or NADP+ as an acceptor and acts on the donor CH-OH group, and can catalyze the oxidation of D-lactate to pyruvate. D-Lactate dehydrogenase widely exists in bacteria and fungi, and is often used in biochemical research[1].
(S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(3-cyanophenyl)propanoic acid is a phenylalanine derivative[1].
Antiproliferative agent-15 is an anticancer agent. Antiproliferative agent-15 shows antiproliferative activity against human colon (HCT116 and HCT15) and brain (LN-229 and GBM-10) cancer cell lines[1].
Androgen receptor antagonist 3 (Compound C18) is an androgen receptor (AR) antagonist with an IC50 of 2.4 μM. Androgen receptor antagonist 3 shows anticancer activities[1].
Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.IC50 value: Target: D2DR/D4DR; 5-HT receptorin vitro: In the presence of Loxapine, [3H]ketanserin binds to 5-HT2 receptor in Frontal cortex of brain in human and bovine with ki value of 6.2 nM and 6.6 nM, respectively. Loxapine has the rank order of potency for the various receptors appears to be as follows:5-HT2≥D4>>>D1>D2 in comparing competition experiments involving the human membranes [1]. Loxapine 0.2 μM, 2 μM and 20 μM reduces IL-1beta secretion by LPS-activated mixed glia cultures after 1 and 3 days of exposure. Loxapine in concentrations of 0.2 μM, 2 μM and 20 μM reduces IL-2 secretion in mixed glia cultures after 1 and 3 days of exposure, and additionally Loxapine decreases IL-1beta and IL-2 secretion in LPS-induced microglia cultures in concentrations of 2 μM, 10 μM and 20 μM [2].in vivo: Loxapine (5 mg/kg) induces a very significant reduction (more than 50%) of serotonin (S2) receptor density after 4 weeks or 10 weeks of daily injection in the rat. Loxapine (5 mg/kg) does not change dopamine receptor density but greatly reduces serotonin receptor density by 47% in the brain of rats [3].
Kv3 modulator 3 (Compound 4) is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels extracted from patent WO2017098254A1, compound 4, has analgesic activity for use in the prophylaxis o or treatment of pain[1].
Goserelin (ICI 118630) acetate is an injectable gonadotropin releasing hormone superagonist (GnRH agonist).IC50 value:Target: GnRH agonistGoserelin is used to treat hormone-sensitive cancers of the breast (in pre- and peri- menopausal women) and prostate, and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty. It may also be used in the treatment of male-to-female transsexuals and is favoured above other anti-androgens in some countries, such as the UK. It is available as a 1-month depot and a long-acting 3-month depot. Goserelin stimulates the production of the sex hormones testosterone and estrogen in a non-pulsatile (non-physiological) manner.
Procyanidin B1 is a polyphenolic flavonoid isolated from commonly eaten fruits, binds to TLR4/MD-2 complex, and has anti-inflammatory activity.
Ibandronic acid is a highly potent nitrogen-containing bisphosphonate used for the treatment of osteoporosis.Target: OthersIbandronate (1.25-2 μM) significantly reduces endothelial cell growth, while ibandronate (2 μM) also significantly reduces capillary-like tube formation and increases apoptosis of endothelial cells. Ibandronate (< 100 μM) dose-dependently increases VEGF expression in endothelial cells [1]. Ibandronate (< 100 μM) inhibits growth of both prostate cancer cell lines (LNCaP and PC-3) in a dose dependent manner [2].Ibandronate administered either daily (2.5 mg) or intermittently (20 mg every other day for 12 doses every 3 months) significantly reduces the risk of new morphometric vertebral fractures by 62% and 50% (p = 0.0006), respectively, in osteoporotic women after 3 years' treatment. Ibandronate administered either daily (2.5 mg) or intermittently (20 mg every other day for 12 doses every 3 months) significantly and progressively increases BMD of lumbar spine by 6.5% and 5.7%, respectively, in osteoporotic women after 3 years' treatment [3]. Ibandronate (< 125 mg/kg s.c.) results in a dose dependent increase in bone mineral density (BMD), trabecular bone volume and trabecular number, load to failure (Fmax), and yield load in long bones and vertebrae in ovariectomized rats, and increased trabecular separation in ovariectomized rats is fully prevented by all doses [4].
3-Hydroxy-2-(palmitoyloxy)propyl stearat is a non-volatile compound. 3-Hydroxy-2-(palmitoyloxy)propyl stearat can be isolated from less polar fractions of the brown macroalga Fucus virsoides J. Agardh. This part of the substance has a good ability to scavenge free radicals and has a protective effect on the oxidative stress induced by hydrogen peroxide in zebrafish embryos[1].
DAF 2DA is most widely probe for NO measurement.