TMX-201 is a TLR7 ligand-phospholipid conjugate. TMX-201 shows potent immune stimulatory activity. TMX-201 can be used for breast cancer and melanoma research[1].
1-Methyl-2'-O-methylinosine is a purine nucleoside analog. 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].
PROTAC IRAK3 degrade-1 is a potent and selective degrader of IRAK3 (IC50 = 5 nM).
Octan-2-yl 2-cyanoacrylate is a cyanoacrylate compound widely used in industry and medicine as a fast-curing glue or tissue adhesive[1].
Carboxyebselen (HOOC-Ebs) is a potent and selective inhibitor of endothelial nitric oxide synthase (eNOS)[1].
Tubulysin D is one of the most potent derivatives among the tubulysins isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin D is a novel tetrapeptide that displays potent antitumor activity and leads to cell cycle arrest and apoptosis by inhibiting tubulin polymerization with an IC50 of 1.7 μM[1]. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[2].
PKH 26 is a lipophilic membrane dye and widely used to determine cell proliferation in heterogeneous cells by flow cytometry. It is a red‐fluorescent dye (Ex/Em=551/567nm)[1][2].
Desvenlafaxine-d6 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity[1][2][3]. 2-Methoxycinnamaldehyde inhibits proliferation and induces apoptosis by mitochondrial membrane potential (ΔΨm) loss, activation of both caspase-3 and caspase-9[2]. 2-Methoxycinnamaldehyde effectively inhibits platelet-derived growth factor (PDGF)-induced HASMC migration[3].
Styraxlignolide F is a natural compoundisolated from Styrax japonica.
5’-O-(4,4’-Dimethoxytrityl)-3’-O-t-butyldimethylsilyl adenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Xylotetraose is a hydrolysis product of Xylan[1]. Xylan is a polysaccharide made from units of xylose and contains predominantly β-D-xylose units linked as in cellulose[2]. Xylotetraose can be used for enzyme biochemical analysis[1][3][4].
KRAS inhibitor-16 (compound 3-11) is a potent KRAS G12C inhibitor with an IC50 of 0.457 µM. KRAS inhibitor-16 shows p-ERK inhibition activities with IC50s of 3.06, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-16 has the potential for the research of pancreatic, colorectal, and lung cancers[1].
Complanatin I is a natural product that can be isolated from Astragalus complanatus[1].
Aglain C is isolated from A. ponapensis. Aglain C enhances the NF-kB inhibitory activity[1].
ISIS 329993 (ISIS-CRPRx) is an antisense oligonucleotide targeting to C-reactive protein (CRP). ISIS-CRPRx?has been tested in a rodent model of rheumatoid arthritis (RA) and was shown to improve the clinical signs of arthritis
RORγ-IN-1 is a RORγ inhibitor extracted from patent US 9481674 B1, has a Ki of <100 nM.
NOT Receptor Modulator 1 is a nuclear receptor NOT modulator extracted from patent WO 2008034974 A1, Example 39 in table1.
Dihydrobupropion-d9 is the deuterium labeled Dihydrobupropion[1].
Neorauflavene is a phenolic neorautanenia isoflavanoid isolated from Neorautanenia edulis. Neorauflavene shows antibacterial activities against E. faecalis, S. suis, S. agalactiae, P. aeruginosa, B. subtilis, and R. anatipestifer[1][2].
Glycyl-DL-aspartic acid (Gly-DL-Asp) is an aspartate derivative that can be used for amino acids synthesis[1].
Bivalirudin Trifluoroacetate is a synthetic 20 residue peptide which reversibly inhibits thrombin.IC50 Value:Target: thrombinin vitro: Eptifibatide (8 mg/mL) added together with a low (70 ng/mL) concentration of bivalirudin (a direct thrombin inhibitor) effectively (approximately 90%) reduced platelet aggregation induced by thrombin (0.2 U/mL) [1]. In thrombin generation assay (TGA), bivalirudin had no effect on these parameters up to 10 μmol/l [2]. Bivalirudin-facilitated binding of MPO to BAEC resulted also in functional changes in terms of increased NO consumption as well as enhanced MPO-mediated redox modifications [3].in vivo: The use of bivalirudinprevented further increase in antiheparin/PF4 antibody IgG levels in rats [4]. Three animals in the 500-mg/kg/24 h group, and 7 animals in the 2000-mg/kg/24 h group in the toxicokinetic assessment phase of the study were found dead or euthanized in extremis (following blood sampling). Plasma concentrations of bivalirudin appeared to be linear and dose independent [5].Clinical trial: Antithrombotic Effects of Ticagrelor Versus Clopidogrel . Phase 4
5’(R)-C-Methylcytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
KRAS G12C inhibitor 54 (Compound 1) is a KRAS G12C inhibitor[1].
1-Bromoicosane-d3 is the deuterium labeled 1-Bromoicosane[1].
Thymus peptide C is a hormonal drug, derived from the thymus glands of young calves and acts as a substitute for the physiological functions of the thymus.
2-Bromo-1,3-difluorobenzene-d3 is the deuterium labeled 2-Bromo-1,3-difluorobenzene[1].
Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2 receptor blocker(Ki= 0.16 nM) and a potent dopamine D2 receptor antagonist(Ki= 1.4 nM). IC50 Value: 0.16 nM (Ki for 5-HT2 receptor); 1.4 nM (Ki for dopamine D2 receptor ) [1]Target: 5-HT2 receptor; D2 receptorRisperidone is an atypical antipsychotic drug which is mainly used to treat schizophrenia (including adolescent schizophrenia) and schizoaffective disorder. Risperidone has excellent oral activity, a rapid onset, and a 24-h duration of action.in vitro: Risperidone is serotonin 5-HT2 receptor blockade as shown by displacement of radioligand binding (Ki: 0.16 nM), activity on isolated tissues (EC50: 0.5 nM). Risperidone is also a potent dopamine D2 receptor antagonist as indicated by displacement of radioligand binding (Ki: 1.4 nM), activity in isolated striatal slices (IC50: 0.89 nM) [1]. Risperidone increased the production of IL-10 and MDC as well as the proinflammatory cytokines, such as IL-6, IL-8, and TNF-α, but decreased the production of IP-10 and IL-12. Furthermore, the exposure of DCs to risperidone led to lower IFN-γ production by T-cells [2].in vivo: Risperidone has the antagonism of peripherally (ED50: 0.0011 mg/kg) and centrally (ED50: 0.014 mg/kg) acting 5-HT2 receptor agonists in rats and antagonism of peripherally (ED50: 0.0057 mg/kg in dogs) and centrally acting D2 receptor agonists (ED50: 0.056-0.15 mg/kg in rats) [1]. Long-Evans rats received daily subcutaneous injections of vehicle or 1 of 2 doses of risperidone (1.0 and 3.0 mg/kg per day) from postnatal Days 14 to 42. Weight gain during development was slightly yet significantly reduced in risperidone-treatedrats. In the first 2 experiments, early-life risperidone administration was associated with increased locomotor activity at 1 week postadministration through approximately 9 months of age, independent of changes in weight gain [3].Toxicity: The changes in the reproductive system (uterus, ovary, vagina, cervix, and mammary gland) were considered secondary to the prolactin elevation, and the congestion of spleen was related to risperidone [4].
Dalbergin is a composition of the extract from the Dalbergia Sissoo Linn. knot wood. Dalbergin demonstrats notable antioxidant ability[1].
Terizidone is an antibacterial agent, and shows bacteriostatic activity. Terizidone can be used in tuberculosis (TB) research[1].