Tubeimoside I(Lobatoside-H) is an extract from Chinese herbal medicine Bolbostemma paniculatum (MAXIM.) FRANQUET (Cucurbitaceae) has been shown as a potent anti-tumor agent for a variety of human cancers.IC50 value:Target: Anticancer natural compoundin vitro: TBMS I inhibited the proliferation of both HepG2 and L-02 cells in a dose- and time-dependent manner, but HepG2 cells appeared more sensitive to the agent. When exposed to TBMS I for 24, 48 and 72 h, IC50 for HepG2 cells versus L-02 cells were 15.5 vs. 23.1, 11.7 vs. 16.2, 9.2 vs. 13.1 (μM, p<0.01), respectively. TBMS I induced cell shrinkage, nuclear condensation and fragmentation, cell cycle arrest at the G2/M phase, mitochondrial membrane disruption, release of cytochrome c from the mitochondria, activation of caspase 3 and 9, and shifting Bax/Bcl-2 ratio from being anti-apoptotic to pro-apoptotic, all indicative of initiation and progression of apoptosis involving mitochondrial dysfunction [1]. TBMS1-induced molecular events were related to mitochondria-induced intrinsic apoptosis and P21-cyclin B1/cdc2 complex-related G2/M cell cycle arrest [2]. TBMS1 combined with CDDP promoted cell apoptosis, decreased proliferation activity and increased cytosolic Ca2+ levels. Bcl-2 protein expression was down-regulated but Bax was up-regulated. Moreover, GST-π mRNA and protein expression were decreased. TBMS1 reduced the resistance of the cells to CDDP-induced cytotoxicity [4]. Treatment with TBMS1 resulted in dose- and time-dependent inhibition of proliferation, led to arrest in phase G2/M of the cell cycle and increased the levels of intracellular Ca2?. Furthermore, TBMS1 up-regulated the levels of the glucose-regulated protein 78/immunoglobuin heavy chain binding protein (GRP78/Bip), C/EBP homologous protein (CHOP), Bax, and cleaved caspase-3 and down-regulated the levels of Bcl-2 [5].in vivo: TBMS1 significantly inhibited the production of the pro-inflammatory cytokines, TNF-α, IL-6 and IL-1β in vitro and in vivo. Pretreatment with TBMS1 markedly attenuated the development of pulmonary edema, histological severities and inflammatory cells infiltration in mice with ALI [3].
Lactate (Lactate acid) is the product of glycolysis. Lactate is produced by oxygen lack in contracting skeletal muscle in vivo, and can be removed under fully aerobic conditions. Lactate can be as a hemodynamic marker in the critically ill[1][2].
17α-Neriifolin is a compound isolated from a methylene chloride extract of the seeds of Cerbera odollam[1].
Fmoc-Ser-OH is a serine derivative[1].
N-(4-Nitrobenzoyl)glycine is a Glycine (HY-Y0966) derivative[1].
Tau Peptide (337-368) (Repeat 4 Domain) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development[1].
Tafluprost(AFP-168) is an anti-glaucoma prostaglandin (PG) analog.Target:OthersTafluprost showed significant IOP-lowering effects without any safety concerns in patients with various types of glaucoma and OH in daily clinical practice and tafluprost is highly effective in any therapeutic patterns [1]. Tafluprost with reduced BAK has potential as a superior antiglaucoma drug, not only for its IOP-lowering effect, but also for its good corneal safety profile [2]. Tafluprost single-use vials treatment was effective in reducing IOP over the 3 years of this study, but visual field performance worsened by 10.3%-13.8% in patients with normal-tension glaucoma. Safety was satisfactory [3].
N-Pivaloyl-L-tyrosine is an N-pivaloyl amino acid ester.
(4-Fluorophenyl)methanol-d6 is the deuterium labeled (4-Fluorophenyl)methanol[1].
Azepan-2-one-d10 is the deuterium labeled Azepan-2-one[1].
Mirin is a small-molecule inhibitor of MRN (Mre11, Rad50, and Nbs1) complex.Target: in vitro: Mirin was shown to block Mre11 exonuclease activity and MRN-dependent ATM activation, and to inhibit the ionizing radiation-induced G2/M checkpoint and homologous recombination in mammalian cells. Mirin inhibition of ATM activation is independent of Mre11 nuclease inhibition since the M(HN)RN and M(HL/DV)RN mutant complexes are inhibited equivalently to the wild-type enzyme despite the fact that they are nuclease-deficient. The effects of Mirin have been ascribed to its effects on Mre11 nuclease activity, but as we show here, Mirin is inhibitory of MRN function independent of the nuclease activity of the complex. [2] Addition of the Mre11 inhibitor Mirin to egg extracts and mammalian cells reduces RCC1 association with mitotic chromosomes. HeLa cells expressing Histone H2B-EYFP were treated with Mirin (25 or 50 μM), and mitotic progression was immediately monitored using live cell imaging. Although Mirin-treated cells were able to congress chromosomes to the metaphase plate with similar kinetics as untreated cells, a significant fraction of Mirin-treated cells paused for extended periods of time in a metaphase-like stage without anaphase onset . [1]
Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload.
Ternatin B4 is an anthocyanin isolated from the flowers of Clitoria ternatea L. (Leguminosae)[1].
N-Boc-Phe-Leu-Phe-Leu-Phe (Boc-FLFLF) is a formyl peptide receptor 1 (FPR1) antagonist, which increases pain effects and inhibits antinociceptive activity of annexin[1][2].
4-Methylumbelliferyl palmitate is an excellent fluorophore for measuring acid lipase in human leukocytes. Acidity and solvent have important influence on its fluorescence. 4-Methylumbelliferyl palmitate exists mainly as neutral molecular form which can be produced strong fluorescence at 445 nm in near neutral aqueous solutions, and exist mainly as anion form which can be produced stronger fluorescence at 445 nm in weak alkaline solutions[1][2].
(-)-Heraclenol is a derivative of furocoumarin isolated from Ducrosia anethifolia. (-)-Heraclenol shows antiproliferative and cytotoxic activities on cancer cell lines[1].
2,3-Didehydrosomnifericin is one of withanolides found in Withania somnifera[1].
Hancinone C (compound 2) is a natural product that can be found in Piper hancei[1].
7,4'-Dihydroxyhomoisoflavane is a natural antioxidant. 7,4'-Dihydroxyhomoisoflavane has ABTS radical-scavenging capacity with an IC50 of 0.22 mg/mL[1].
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively[1]. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer[1][2][4].
4,5-Dihydroblumenol A is a norisoprenoid, that can be isolated from Pavonia multiflora A. ST-HIL. (Malvaceae)[1].
Benzyldimethylstearylammonium chloride, a quarternary ammonium compound, exerts no selective embryopathic activity[1].
WAY-637940 is an active molecule.
Urodilatin is an analogue of ANF-(99-126). Urodilatin is a diuretic-natriuretic regulatory peptide. Urodilatin can be used for research of acute renal failure, congestive heart failure, and bronchial asthma, etc[1].
H-His-Lys-OH is adipeptide.
CV-6209 is a potent antagonist of platelet activating factor (PAF). CV-6209 inhibits the PAF-induced aggregation of rabbit and human platelets, with IC50s of 75 nM and 170 nM, respectively. CV-6209 can inhibit PAF-induced hypotension in rats[1].
L-2-Aminooxy-3-phenylpropanoic acid is a potent inhibitor of L-phenylalanine ammonia-lyase[1].
H-Tyr(H2PO3)-OH is a tyrosine derivative[1].
SIGSLAK has the active site of E. coli penicillin-binding protein 1b[1].
m-Tolylacetic acid (3-Methylbenzeneacetic acid) is a hydroaromatic dicarboxylic acids excreted in the urine as metabolite of tolueneacetic acid[1].