(-)-Praeruptorin A is a nature product that could be isolated from the roots of Peucedanum praeruptorum Dunn. (-)-Praeruptorin A relaxes ileum and tracheal smooth muscles by activating NO/cGMP signaling pathway. (-)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca2+-influx blocker[1].
Novel Potent Inhibitor of the Protein Phosphatase Slingshot
CD3254 a potent and selective retinoid-X-receptor (RXR) agonist[1].
Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets[1]. Calpeptin is also an inhibitor of cathepsin K[2].
Pyrrole-2-carboxaldehyde has vibrational and electronic characteristics used to establish the existence of dimeric form in solid phase and monomeric form in solution phase[1].
Rizatriptan Benzoate(Maxalt) is a 5-HT1 agonist triptan drug for the treatment of migraine headaches.Target: 5-HT1 agonist Rizatriptan Benzoate(Maxalt) is a 5-HT1 agonist triptan drug for the treatment of migraine headaches. It is believed to work by narrowing the blood vessels around the brain. Rizatriptan also reduces the substances in the body, which can also reduce headache pain, nausea, sensitivity to light and sound and other migraine symptoms.Rizatriptan was rapidly absorbed with a median tmax of 1.3 h (range 1-3 h) vs a tmax for sumatriptan of 2.5 h (range 1-4 h, P < 0.001). Administration of either rizatriptan or sumatriptan produced maximal mean elevations of 5-10 mmHg in systolic and diastolic blood pressures without effect on heart rate; the changes occurred sooner following rizatriptan, consistent with more rapid absorption. Both rizatriptan and sumatriptan provoked mild increases in serum growth hormone without any effect on serum prolactin concentrations. The most commonly reported symptom following rizatriptan was drowsiness.
Amino-PEG10-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Tenuazonic acid, belonging to tetramic acids that are the largest family of natural products, is a putative nonhost-selective mycotoxin isolated from Alternaria alternate[1]. Tenuazonic acid blocks electron transport beyond primary quinone acceptor (QA) by interacting with D1 protein and it is a broad-spectrum and effective photosystem II (PSII) inhibitor[2].
4-Methylpentanoic acid-d11 is the deuterium labeled 4-Methylpentanoic acid[1]. 4-Methylpentanoic acid (Isocaproic Acid) is a Short chain fatty acid (SCFA)[2].
14-Deoxy-11,12-didehydroandrographiside is a compound isolated from A. paniculate[1].
Polysaccharidase (Tremella polysaccharide), one of the fungus polysaccharides, possesses immunity enhancing capabilities. Polysaccharidase has the potential for leukopenia induced by chemotherapy and radiotherapy research[1][2].
Alatrofloxacin, the parenteral prodrug of Trovafloxacin, is a fluoronaphthyridone which contains an L-alanyl-L-alanyl salt. Alatrofloxacin functions similar to other fluoroquinolone antibiotics in that it not only has antibiotic activity to kill invading organisms by interfering with DNA synthesis, it possesses immunosuppressive activity[1].
INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity[1].
Denecimig (Mim8) is a novel activated coagulation factor VIII-mimetic human bispecific antibody with anti-FIXa and anti-FX arms that potently stimulates FX activation resulting in efficacious haemostasis in vitro and in vivo[1].
CSF1R-IN-12 is a potent inhibitor of CSF1R. Colony stimulating factor 1 (CSF-1, also known as macrophage colony stimulating factor, M-CSF) is an important growth factor that controls bone marrow progenitor cells, monocytes, macrophages, and giants. CSF1R-IN-12 has the potential for the research of cancer diseases (extracted from patent WO2019134661A1, compound 1)[1].
F-17 is a potential inhibitor of virulence factor. F-17 shows very significant inhibitory effect on biofilm, elastase, pyocyanin, and swarming motility. F-17 also shows a good binding effect on LasR and PqsR. F-17 has no obvious cytotoxicity[1].
Adrenomedullin (porcine) is a peptide that regulates vasodilation. Adrenomedullin (porcine) induces endothelium-dependent relaxation in rat aorta with IC50 value of 2.4 nM. Adrenomedullin (porcine) induces endothelium-independent relaxation of porcine coronary arteries with an IC50 of 27.6 nM[1].
Tecastemizole (Norastemizole), a major metabolite of Astemizole, is a potent and selective H1 receptor antagonist. Tecastemizole shows anti-inflammatory activities[1].
PF-1163B is an antifungal antibiotic[1].
1,8-Dimethylnaphthalene-d12 is the deuterium labeled 1,8-Dimethylnaphthalene[1].
(±)-Trolline ((±)-Oleracein E), an isoquinoline alkaloid, exhibits antibacterial activity against respiratory bacteria and antiviral activity against influenza virus A and B. (±)-Trolline significantly induces HSC apoptosis. (±)-Trolline can be used for the research of liver fibrosis[1].
hCAIX-IN-14 (compound 5a) is a potent inhibitor of human CA IX with a Ki value of 134.8 nM[1].
BMS-604992 (EX-1314) is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 demonstrates high-affinity binding (Ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 can stimulate food intake in rodents[1].
gamma-secretase modulator 3 is a gamma-secretase modulator.
Br-Boc-C2-azido is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
EPZ004777 is a potent, selective DOT1L inhibitor with an IC50 of 0.4 nM.
Triciribine phosphate (TCN-P) inhibits amidophosphoribosyltransferase by an allosteric mechanism which affects the first committed step of de novo purine biosynthesis. Triciribine phosphate also inhibits IMP dehydrogenase which is the first committed step of guanosine nucleotide synthesis. Tricilibine phosphate does not affect ligase activity[1].
Neurotensin (1-8) is a biologically active peptide.
11-Hydroxysugiol regulates the SUMOylation of intracellular receptors by modulating RARα and vitamin D3 receptor (VDR)[1].
Altechromone A is a natural product that can be isolated from Polygonum cuspidatum[1].