PSMα3 is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. PSMα3 penetrates and modulates human monocyte-derived DCs by altering the TLR2- or TLR4-induced maturation, inhibiting pro- and anti-inflammatory cytokine production and reducing antigen uptake. PSMα3 is an important toxin released by the most virulent strains of methicillin-resistant Staphylococcus aureus (MRSA)[1][2].
7-Methyl-DL-tryptophan (7-Methyltryptophan) is an amino acid derivative, which is a key precursor for biosynthesis of many non-ribosomal peptide antibiotics. 7-Methyl-DL-tryptophan plays an important role in synthesis of high-efficiency antibacterial agents and analogues thereof[1].
β-Estradiol 17-hemisuccinate is a synthetic derivative of estradiol (HY-B0141)[1].
Bremzalerbart is a human IgG4 antibody targeting BETVIA, the major birch pollen allergen Bet v 1-A[1].
DL-Penicillamine [(±)-Penicillamine] is a copper chelating agent. DL-Penicillamine has antidotal effects in thallotoxicosis rats when co-treated with Prussian blue (HY-106594A). DL-Penicillamine can cause pyridoxine deficiency and then induce optic axial neuritis. DL-Penicillamine can also depress primary immune response[1][2][3].
IR-820 (New Indocyanine Green) is an infrared blood pool contrast agent. IR-820 also is normally used as a laser and near-infrared dye to detect and quantify diseased tissue in live animals[1].
Acetagastrodin (compound 4) is an intermediate for the synthesis of DBPG (an antioxidant from Origanum vulgare)[1].
Steroid sulfatase -IN-2 is an active steroid sulfatase (STS) inhibitor with an IC50 value of 109.5 nM. Steroid sulfatase-IN-2 can be used for the research of hormone-dependent cancers, such as estrogen-dependent breast and endometrial cancer[1].
Ibandronate Sodium is a highly potent nitrogen-containing bisphosphonate used for the treatment of osteoporosis.Target: OthersIbandronate (1.25-2 μM) significantly reduces endothelial cell growth, while ibandronate (2 μM) also significantly reduces capillary-like tube formation and increases apoptosis of endothelial cells. Ibandronate (< 100 μM) dose-dependently increases VEGF expression in endothelial cells [1]. Ibandronate (< 100 μM) inhibits growth of both prostate cancer cell lines (LNCaP and PC-3) in a dose dependent manner [2].Ibandronate administered either daily (2.5 mg) or intermittently (20 mg every other day for 12 doses every 3 months) significantly reduces the risk of new morphometric vertebral fractures by 62% and 50% (p = 0.0006), respectively, in osteoporotic women after 3 years' treatment. Ibandronate administered either daily (2.5 mg) or intermittently (20 mg every other day for 12 doses every 3 months) significantly and progressively increases BMD of lumbar spine by 6.5% and 5.7%, respectively, in osteoporotic women after 3 years' treatment [3]. Ibandronate (< 125 mg/kg s.c.) results in a dose dependent increase in bone mineral density (BMD), trabecular bone volume and trabecular number, load to failure (Fmax), and yield load in long bones and vertebrae in ovariectomized rats, and increased trabecular separation in ovariectomized rats is fully prevented by all doses [4].
Neoline, the active ingredient of processed aconite root (PA), alleviated oxaliplatin-induced peripheral neuropathy in mice. Neoline can be used as a marker compound to determine the quality of the PA products for the treatment of neuropathic pain[1].
Quercetin-3-O-sambubioside is a monomeric compound found in Eucommia ulmoides male flowers. Quercetin-3-O-sambubioside promotes the stimulation of the nerve center. Antioxidant and anticancer activities[1][2].
6-Aminonicotinamide, a potent antimetabolite of nicotinamide, is competitive NADP+-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) inhibitor (Ki=0.46 μM). 6-Aminonicotinamide interferes with glycolysis, resulting in ATP depletion and synergizes with DNA-crosslinking chemotherapy drugs, such as Cisplatin, in killing cancer cells[1][2][3][4].
Thevetin A is a thevetia cardiac glycoside. Thevetin A can be isolated from the methanol extract of the seeds of Cascabela thevetioides[1].
[Asn23] β-Amyloid (1-40), Iowa mutation is a biological active peptide. (Several mutations in the beta amyloid precursor gene cause autosomal dominant Alzheimer's Disease in a number of kindreds. The Iowa mutation, where Asp 23 is replaced with Asn, is associated with severe cerebral amyloid beta-protein angiopathy (CAA). The affected individuals share a missense mutation in APP at position 694. The mutated beta-amyloid peptide aggregates more rapidly and forms toxic fibrils.)
7-Hydroxymethotrexate-d3 is the deuterium labeled 7-Hydroxymethotrexate. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis[1][2].
PHGDH-inactive has no activity against PHGDH and serves as a negative control of NCT-502 and NCT-503[1].
Methimazole(Tapazole, Northyx) is an antithyroid medicine.Target: OthersMethimazole is an antithyroid drug, and part of the thioamide group. Like its counterpart propylthiouracil, a major side effect of treatment is agranulocytosis. Methimazole is a drug used to treat hyperthyroidism, a condition that occurs when the thyroid gland begins to produce an excess of thyroid hormone. The drug may also be taken before thyroid surgery to lower thyroid hormone levels and minimize the effects of thyroid manipulation. Additionally, Methimazole is used in the veterinary setting to treat hyperthyroidism in cats.Methimazole inhibits the enzyme thyroperoxidase, which normally acts in thyroid hormone synthesis by oxidizing the anion iodide (I-) to iodine (I0), facilitating iodine's addition to tyrosine residues on the hormone precursor thyroglobulin, a necessary step in the synthesis of triiodothyronine (T3) and thyroxine. It does not inhibit the action of the sodium-dependent iodide transporter located on follicular cells' basolateral membranes. Inhibition of this step requires competitive inhibitors such as perchlorate and thiocyanate.It acts at CXCL10.
(±)-trans-4-Hydroxy-2-hexenal-5,5,6,6,6-dd5 Dimethyl Acetal is the deuterium labeled (±)-trans-4-Hydroxy-2-hexenal Dimethyl Acetal[1].
Allylestrenol, a synthetic sexualsteroid, is used worldwide in case of endangered pregnancies.
DL-α-Tocopherol acetate is a vitamin E derivative which is often included in the formulations of enteral nutrition.
TOOS, a Trinder's reagent, is a novel highly water-soluble aniline derivative; are widely used in diagnostic tests and biochemical tests.
Dantrolene-13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
N,N-Dimethylacetamide-d3 is the deuterium labeled N,N-Dimethylacetamide[1]. N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent[2].
1-Bromononane-d3 is the deuterium labeled 1-Bromononane[1].
Tetrazine-Amine is a tetrazine linker that can be used to covalently label live cells through a cycloaddition[1][2].
Octanoyl coenzyme A lithium is a fatty acyl coenzyme A derivative. Octanoyl coenzyme A lithium can inhibit citrate synthase (CS) and glutamate dehydrogenase (GDH) with IC50 values of 0.4-1.6 mM[1].
Sylvestroside I is an iridoid isolated from Acicarpha tribuloides[1].
Kobe2601 is a Kobe0065 (HY-15716) analogue. Kobe2601 can be used to probe the Kobe family of compounds' mechanism of action[1].