Bz-RGFFL-4MβNA (Bz-Arg-Gly-Phe-Phe-Leu-4MβNA) is a peptide and can be used fluorogenic substrate[1].
7-Fluorobenzofurazan-4-sulfonic acid ammonium is a fluorescent label. 7-Fluorobenzofurazan-4-sulfonic acid ammonium can be used for detecting dissolved thiol-disulfide (e.g., Cys, GSH)[1].
Vinorelbine is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. It works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM.
Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator.The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R). Sequence: Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2.
Firazorexton is a potent orexin type 2 receptor (OX2R) agonist (patent WO2019027058A1, example 395)[1].
GW7604 is an antiestrogen. GW7604 is the metabolite of GW5638, which is a high affinity estrogen receptor (ER) antagonist[1].
Isochavicine is an alkaloids that can be isolated from Piper retrofractum. Isochavicine inhibits the seedling growth of cress with I50 values of 11 μM[1].
Denudatine, is primarily isolated from plants of the genera Aconitum and Delphinium[1]. Denudatine has effects on action potential of ventricular fibers and inhibits arrhythmogenic action of aconitine[2].
Polygalacin D2 is a saponin isolated from Platycodon grandiflorum[1].
2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-6-methoxy-9H-purine 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].
1,2,4-Triazine-3,5-dione 2-β-D-xylopyranoside 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].
Iminostilbene is a a chemical precursor of carbamazepine[1].
9-epi-Blumenol C β-D-glucopyranoside (9-epi-Blumenol C glucoside) is a natural product isolated from Stachys byzantina[1].
Testosterone tridecanoate is a prodrug of testosterone. Testosterone is the primary male sex hormone and an anabolic steroid.
Angiogenesis inhibitor 3 (compound 8) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 3 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.00 and 0.71 μM. Angiogenesis inhibitor 3 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 3 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 3 inhibits the angiogenesis in zebrafish embryos[1].
Prostaglandin E2 is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for ADC with antitumor activity by using the tubulin inhibitor, MMAF, linked via cathepsin cleavable MC-Val-Cit-PAB.
FzM1.8 derives from FzM1, is an allosteric agonist of FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K[1].
Talipexole (B-HT920) is a dopamine agonist that has been proposed as an antiparkinsonian agent.Target: Dopamine ReceptorB-HT920 is a selective alpha 2-adrenoceptor agonist. The effects of B-HT920 have been specified using the alpha-adrenergic antagonists yohimbine and prazosin and the dopamine antagonist haloperidol. Yohimbine could not antagonize any of the actions of B-HT920. Pretreatment with prazosin showed a decrease in the loss of body weight caused by B-HT920, while pretreatment with yohimbine showed that B-HT920 induced an increased loss in body weight. These data suggest that B-HT920 under certain conditions exerts dopamine-agonistic actions in stimulating locomotor activity and alpha 1-adrenergic actions in inducing salivation and enhanced loss of body weight [1]. Concomitant treatment with talipexole, an anti-parkinsonian drug, inhibited MPTP-induced autolysis and individual death in a concentration-dependent manner. Pramipexole showed a similar protective effect. In addition, post-treatment with talipexole at 1 hr after MPTP completely inhibited MPTP-induced individual death. Although MPTP treatment caused 30% of the planarians to undergo autolysis and individual death within 12 hr, post-treatment with talipexole even at 12 hr completely rescued the remaining 70% of the planarians from death. These results suggest that the MPTP-treated planarian may be useful as a novel parkinsonian model in which talipexole has a protective effect even in the case of post-treatment [2].
N-p-Tosylglycine is a Glycine (HY-Y0966) derivative[1].
(±)-Naproxen-d3 ((Rac)-Naproxen-d3) is the deuterium labeled (±)-Naproxen. (±)-Naproxen is a non-steroidal anti-inflammatory drug (NSAID)[1].
Tetraarginine (RRRR), consisting of four arginines, is used in cell-penetrating peptide-based gene delivery vehicles[1].
Octyl β-D-thioglucopyranoside is a non-ionic detergent that can be used in the field of membrane biochemistry. Octyl β-D-thioglucopyranoside has the ability to solubilize E. coli membrane proteins[1].
Garenoxacin (BMS 284756) mesylate is an orally active quinolone antibiotic and Garenoxacin mesylate has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes. Garenoxacin mesylate also inhibits Gyrase and TOPO IV[1][2][3][4].
Clopidogrel sulfate is an antiplatelet agent. Specifically, Clopidogrel sulfate inhibits the binding of ADP to its receptors on the membranes of platelet cells, and blocks ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. Clopidogrel sulfate can be used for research of heart disease and stroke[1].
AcBut is a pH cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
A novel potent and metabolically stable tubulin inhibitor that can circumvent the drug efflux pumps responsible for multidrug resistance of existing tubulin inhibitors; demonstrates cytotoxicty in a panel of human metastatic melanoma cell lines harboring major clinically relevant mutations with IC50 of 7-10 nM, disrupts microtubule networks, suppresses anchorage-dependent melanoma colony formation, and impaires cancer cell migration; inhibits tumor growth and reduced lung metastasis in melanoma-bearing mice, also completely inhibits tumor growth in a paclitaxel-resistant xenograft mouse model.
HIV-1 integrase inhibitor 9 (compound 8a) is a potent HIV-1 RNase H inhibitor with an IC50 of 12.3 μM. HIV-1 integrase inhibitor 9 shows an antiviral activity[1].
(2E,6E)-3,7-Dimethyltrideca-2,6-dien-12-yn-1-ol is a isoprenoid analogue[1].