Tetraethylammonium iodide is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
A novel reactivator of wild-type and mutant p53, shows a p53-dependent anti-proliferative activity in human wt and mut p53R280K-expressing tumor cells; enhances p53 transcriptional activity and restores wt-like DNA binding ability to mut p53R280K; inhibits the growth of wt/mut p53-expressing tumors in xenograft mice models, without apparent toxicity.
OPC-163493 is an orally active liver-targeted mitochondrial uncoupling agent. OPC-163493 reduces Δψ and mitochondrial ROS production. OPC-163493 has antidiabetic and cardiovascular beneficial effects. OPC-163493 lowers blood pressure, extends survival, and improves renal function in the rat model of stroke/hypertension[1].
Bis-5,5-Nortrachelogenin is isolated from active extract of root of Wikstroemia indica. Bis-5,5-Nortrachelogenin inhibits nitric oxide (NO) production in a lipopolysaccharide (LPS) and recombinant mouse interferon-γ(IFN-γ) activated murine macrophage-like cell line, RAW 264.7 with an IC50 value of 48.6 mM[1].
Quizalofop-ethyl-d3 is the deuterium labeled Quizalofop-ethyl[1].
Betulin diacetate, a natural diterpene, is an anti-AID agent and also possesses anti-cancer activity[1][2].
Metoprolol is a cardioselective β1-adrenergic blocking agent.Target: β1- adrenergic ReceptorPatients took 50 mg metoprolol twice daily with weekly titration to response or 200 mg twice daily. beta(1)-adrenergic receptor polymorphisms are important determinants of antihypertensive response to metoprolol. In the future, codon 49 and 389 genotypes or beta(1)-adrenergic receptor haplotypes might be used to predict the diastolic blood pressure response to metoprolol in patients with hypertension [1]. Patients were studied at baseline and after each dose titration of metoprolol succinate (at 25, 50, 100, and 200 mg once/day) and immediate-release carvedilol (at 3.125, 6.25, 12.5, and 25 mg twice/day). As assessed by glucose AUC, there was no significant difference in the degree of beta(2)-blockade between metoprolol 200 mg and carvedilol 25 mg. In contrast to these data, the degree of beta(2)-blockade as assessed by potassium AUC was greater for carvedilol compared with metoprolol across all doses [2].
Cyanine 5.5 azide (CY 5.5 azide) is a potent fluorescent dye. Cyanine 5.5 azide can label DNA. Cyanine 5.5 azide can be used for NIR live organism imaging. (λex=684 nm, λem=710 nm)[1][2].
Warfarin(WARF42) is an anticoagulant drug normally used to prevent blood clot formation as well as migration.Target: OthersWarfarin is an anticoagulant normally used in the prevention of thrombosis and thromboembolism, the formation of blood clots in the blood vessels and their migration elsewhere in the body respectively. Warfarin and related 4-hydroxycoumarin-containing molecules decrease blood coagulation by inhibiting vitamin K epoxide reductase, an enzyme that recycles oxidized vitamin K1 to its reduced form after it has participated in the carboxylation of several blood coagulation proteins, mainly prothrombin and factor VII. Despite being labeled a vitamin K antagonist, warfarin does not antagonize the action of vitamin K1, but rather antagonizes vitamin K1 recycling, depleting active vitamin K1 [1, 2].
Hoechst stains are part of a family of blue fluorescent dyes used to stain DNA. Hoechst 33258 is a cell dye for DNA quantitation.IC50 Value:These Bis-benzimides were originally developed by Hoechst AG, which numbered all their compounds so that the dye Hoechst 33342 is the 33342nd compound made by the company. There are three related Hoechst stains: Hoechst 33258, Hoechst 33342, and Hoechst 34580. The dyes Hoechst 33258 and Hoechst 33342 are the ones most commonly used and they have similarexcitation/emission spectra. Both dyes are excited by ultraviolet light at around 350 nm, and both emit blue/cyan fluorescent light around anemission maximum at 461 nm. Unbound dye has its maximum fluorescence emission in the 510-540 nm range. Hoechst dyes are soluble in water and in organic solvents such as dimethyl formamide or dimethyl sulfoxide. Concentrations can be achieved of up to 10 mg/mL. Aqueous solutions are stable at 2-6 °C for at least six months when protected from light. For long-term storage the solutions are instead frozen at ≤-20 °C.The dyes bind to the minor groove of double-stranded DNA with a preference for sequences rich in adenine andthymine. Although the dyes can bind to all nucleic acids, AT-rich double-stranded DNA strands enhance fluorescence considerably.Hoechst dyes are cell-permeable and can bind to DNA in live or fixed cells. Therefore, these stains are often called supravital, which means that cells survive a treatment with these compounds. Cells that express specific ATP-binding cassette transporter proteins can also actively transport these stains out of their cytoplasm.
Condurango glycoside A is an activator of p53. Condurango glycoside A initiates ROS generation and up-regulates p53 expression. Condurango glycoside A induces apoptosis and pre-mature senescence associated with DNA damage in HeLa cells[1].
QNZ shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. EVP4593 is a neuroprotective inhibitor of SOC channel.
Fmoc-D-Thr(PO(OBzl)OH)-OH is a threonine derivative[1].
2,4′-Dichlorobiphenyl-d8 is the deuterium labeled 2,4'-Dichloro-1,1'-biphenyl[1].
Xanthine oxidase-IN-1 is a xanthine oxidase inhibitor extracted from patent WO2008126898A1, page 68, compound example 3, with an IC50 of 6.5 nM.
Lucifer yellow CH (LYC) ammonium is a thiol-reactive fluorescent polar tracer.
β-N-Acetylhexosaminidase is an exoglycosidase that catalyzes the hydrolysis of terminal non-reducing β-N-acetylgalactosamine and glucosamine residues in oligosaccharides for epigenetic applications[1].
L-Tyrosine-13C,15N is the 13C and 15N labeled L-Tyrosine[1]. L-Tyrosine is a non-essential amino acid which can inhibit citrate synthase activity in the posterior cortex[2].
Ro 25-6981 Maleate is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.IC50 value: 9 nM [1]Target: NMDA receptor subtype of NR1C & NR2Bin vitro: Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity [1]. Increasing the concentration of spermidine did not change the efficacy of RO 25-6981 and minimally changed the IC(50) value. Epsilon1Q336R receptors were more inhibited by ifenprodil and RO 25-9681 than wildtype epsilon1 receptors in ligand binding assays but not in functional assays [2].in vivo: Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation [3].
EG00229 is the first small molecule inhibitor of the neuropilin-1 and VEGF-A interaction with an IC50 of inhibition of 8 uM(125I-VEGF binding to PAE/NRP1 cells).IC50 value: 8 uM [1]Target: NRP1/VEGF-A inhibitorEG00229 reduced VEGF-A-induced VEGFR2 tyrosine phosphorylation in HUVECs in a dose-dependent fashion, with a maximum inhibition of 34% at 100 μM. EG00229 also significantly reduced VEGF-A induced migration of HUVECs. caused a partial inhibition of VEGF receptor activity and biological function, consistent with the current model for the role of NRP1 in VEGF function, in which NRP1 is required for optimal signaling and certain biological functions downstream of VEGFR2, particularly migration [1].
Rhombifoline is an alkaloid isolated for the first time from the leaves and stems of A. foetida L[1].
Fmoc-3-(2-quinolyl)-DL-Ala-OH is an alanine derivative[1].
TRK-IN-23 (compound 24b) is a potent and orally active TRK inhibitor with IC50 values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against TRKA, TRKC, TRKAG595R, TRKAF589L, and TRKAG667C, respectively. TRK-IN-23 indues apoptosis of Ba/F3-TRKAG595Rand Ba/F3-TRKAG667C cells[1].
Lauroyl-L-carnitine chloride can be used as an absorption enhancer[1].
Isochenodeoxycholic acid (isoCDCA) is a human fecal bile acid. Isochenodeoxycholic acid has cytoprotective against ethanol-induced cell injuries in HepG2 cells. Isochenodeoxycholic acid is a major metabolite of orally administered ursodeoxycholic acid (UDCA)[1].
pTH-Related Protein (1-40) (human, mouse, rat) stimulates calcium uptake in rat intestinal cells through PTHR1 receptor and PKCα/β signaling pathways. pTH-Related Protein (1-40) up-regulates parathyroid hormone 1 receptor (PTHR1) protein, four transcellular calcium transporters, potential vanillin member 6 (TRPV6), calcium-binding protein-D9K (CaBP-D9k), sodium-calcium Exchanger 1 (NCX1) and plasma membrane calcium ATPase 1 (PMCA1)[1].
LANA-DNA-IN-1 is a potent LANA-DNA inhibitor. LANA-DNA-IN-1 has inhibition activity for LBS2, LBS1 and LBS3 with IC50 values of 8 μM, 9μM and 8μM. LANA-DNA-IN-1shows against wild-type LANA with IC50 value of 53 μM. LANA-DNA-IN-1 can be used for the research of infection[1].
6-(Methylthio)purine (6-Methylmercaptopurine) is a small molecule that can be used for compound synthesis[1].
2',3'-Dehydrosalannol is a potent antibacterial agent. 2',3'-Dehydrosalannol shows antibacterial activity against K. pneumonia ATCC 13883, P. aeruginosa ATCC 27853, S. aureus ATCC 25922, E. coli ATCC 11775, and E. faecalis ATCC 10541, with MIC values of 0.78, 1.56, 1.56, 6.25, and 25 µg/mL, respectively[1].
AGX51 is a first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability. AGX51 inhibits pathologic ocular neovascularization[1].