NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3), and a cardiotonic agent with vasodilator properties.
Antofloxacin hydrochloride is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin hydrochloride shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin hydrochloride is a weak, reversible inhibitor of CYP1A2 for the treatment of infections caused by a diverse group of bacterial species[1][2][3].
2,3,4,6-Tetra-O-acetyl-D-mannopyranosyl Fluoride is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Leucomycin tartrate (Kitasamycin tartrate) is a potent 16-membered macrolideantibiotic[1].
4-Butylaniline-d6 is the deuterium labeled 4-Butylaniline[1].
1,2-Dilaurin is a diacylglycerol containing lauric acid at the sn-1 and sn-2 positions. It has been used as an internal standard for the quantification of diglycerides in rat desheathed sciatic nerves. [1] Monomolecular films containing 1,2-dilauroyl-rac-glycerol have been used as substrates to measure surface pressure and the effect of pancreatic procolipase and colipase on porcine pancreatic lipase activity. [2] References: [1]. Zhu, X. and Eichberg, J. 1,2-Diacylglycerol content and its arachidonyl-containing molecular species are reduced in the sciatic nerve of streptozotocin-induced diabetic rats. J. Neurochemistry. 55(3), 1087-1090 (1990).[2]. Wieloch, T., Borgstr?m, B., Piéroni, G. et al. Porcine trypsinogen and its trypsin-activated form: lipid binding and lipase activation on monomolecular membranes. FEBS Express. 128(2), 217-220 (1981).
D-Galactose-13C-5 is the 13C labeled D-Galactose. D-Galactose is a natural aldohexose and C-4 epimer of glucose[1][2][3][4].
ITIC-4F is an indacenodithienothiophene (IDTT)-based postfullerene electron acceptor.ITIC-4F has broad applicability in high-efficiency binary and ternary single-junction as well as tandem polymer solar cells (PSCs)[1].
2-(Benzyl(methyl)amino)ethanol-d4 is the deuterium labeled 2-(Benzyl(methyl)amino)ethanol[1].
RUNX1/ETO tetramerization-IN-1 is a small-molecule inhibitor of RUNX1/ETO tetramerization, exhibits anti-leukemic effect. RUNX1/ETO tetramerization-IN-1 specifically targets to NHR2 of RUNX1/ETO (EC50=0.25 μM), restores gene expression down-regulated by RUNX1/ETO. RUNX1/ETO tetramerization-IN-1 inhibits the proliferation of RUNX1/ETO-depending SKNO-1 cells, and reduces the RUNX1/ETO-related tumor growth in a mouse model[1][2][3].
CFT8634 is a degrader targeting BRD9 extracted from patent WO2021178920A1 compound 173. CFT8634 can be used for the research of synovial sarcoma and SMARCB1-deleted solid tumors[1].
PARP1-IN-6 is a dual tubulin/PARP-1 inhibitor with IC50 values of 0.94 and 0.48 μM, respectively.
(R)-Reticuline is an isomer of Reticuline (HY-N1356). Reticuline displays anti-inflammatory and cardiovascular effects through JAK2/STAT3 and NF-κB signaling pathways. Salutaridine is a key intermediate in morphine biosynthesis. Salutaridine can be converted from (R)-Reticuline in the poppy plant. The conversion system relies on membrane-bound cytochrome P-450 enzymes and also requires reducing cofactors NADPH, molecular oxygen, etc[1][2].
N-Acetyldopamine dimer-2 (compound 2) is a N-acetyldopamine dimer that can be isolated from the yellow powder form Periostracum Cicadae with antioxidant and anti-inflammatory activities. N-Acetyldopamine dimer-2 inhibits oxidized low-density lipoprotein (LDL) oxidation, ROS generation, NO production, and NF-κB activity[1].
CSP1 is a potent and selective ComD1 receptor agonist, with an IC50 of 10.3 nM. CSP1 is a major variants of competence-stimulating peptide (CSP), and it can regulate genetic transformation of S. pneumonia by modulating quorum sensing (QS). CSP1 can act as an antibacterial agent[1][2].
Dichlormid is a herbicide safener. Dichlormid up-regulates expression of ZmGST27 and ZmMRP1 and increases ZmGT1[1][2].
STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole (ABZI)-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function[1].
Nω-Propyl-L-arginine (N-omega-Propyl-L-arginine) is a potent, competitive, and highly selective inhibitor of neuronal nitric oxide synthase (nNOS), with a Ki of 57 nM. Nω-Propyl-L-arginine displays a 149-fold selectivity for nNOS over endothelial NOS (eNOS)[1][2].
Ioxaglic acid (P-286) is negatively charged contrast agent, is useful as an inverse indicator for glycosaminoglycan (GAG) used in computed tomography (CT). Ioxaglic acid can be used for imaging of human osteoarthritic cartilage via quantitative assessment of glycosaminoglycan content[1][2].
SSR128129E free acid is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
IPG7236 is a selective CCR8 antagonist. IPG7236 exhibits significant tumor suppression in a mouse xenograft model of human breast cancer. IPG7236 can be used in cancer research[1].
AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc.IC50 value: 20 nM (HER1); 30 nM (HER2) [1]Target: HER1/HER2in vitro: BMS-599626 inhibited HER1 and HER2 with IC50 of 20 and 30 nmol/L, respectively, and was highly selective when tested against a broad panel of diverse protein kinases. Biochemical studies suggested that BMS-599626 inhibited HER1 and HER2 through distinct mechanisms. BMS-599626 abrogated HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50 in the range of 0.24 to 1 micromol/L. BMS-599626 was highly selective for tumor cells that depend on HER1/HER2 and had no effect on the proliferation of cell lines that do not express these receptors. In tumor cells that are capable of forming HER1/HER2 heterodimers, BMS-599626 inhibited heterodimerization and downstream signaling [1]. At the molecular level, in HN-5 cells the agent inhibited the expression of pEGFR, pHER2, cyclins D and E, pRb, pAkt, pMAPK, pCDK1 and 2, CDK 6, and Ku70 proteins. The drug also induced accumulation of cells in the G1 cell cycle phase, inhibited cell growth, enhanced radiosensitivity, and prolonged the presence of γ-H?AX foci up to 24 h after radiation [2].in vivo: BMS-599626 had antitumor activity in models that overexpress HER1 (GEO), as well as in models that have HER2 gene amplification (KPL4) or overexpression (Sal2), and there was good correlation between the inhibition of receptor signaling and antitumor activity [1]. The drug given before and during irradiation improved the radioresponse of HN5 tumors in vivo [2].
Bremelanotide (PT-141) is an analogue of α-melanocyte-stimulating hormone (α-MSH). Bremelanotide activates the mPOA and other hypothalamic and limbic regions of the brain involved in sexual behavior. Bremelanotide can be used for researching hypoactive sexual desire disorders[1].
Influenza HA (110-119) is the 110-119 fragment of influenza virus hemagglutinin that can stimulate Treg cells proliferation[1][2].
N-Arachidonoyl-3-hydroxy-γ-aminobutyric acid is an arachidonoyl amino acid[1].
Ethiprole is an insecticide.Metabolic sulfones are produced faster than Fipronil (HY-B0822) in CYP3A4-expressing cells and in vivo in mouse brain and liver.Ethiprole's sulfide, sulfoxide, sulfone and desulfinyl derivatives have better biological activity[1].
Fulvine is a pyrrolizidine alkaloid isolated from the seeds of Crotalaria fulva. Fulvine is hepatotoxic and can be used to induce hypertensive pulmonary vascular disease in vivo[1].
Cromoglicic acid-d5 is the deuterium labeled Cromolyn[1]. Cromolyn is a mast cell stabilizer. Cromolyn has the potential for the research of bronchial asthma, allergic rhinitis, and certain allergic eye conditions such as vernal conjunctivitis, keratitis, and keratoconjunctivitis[2].
CDK9/10/GSK3β-IN-1 (compound 13c) is a kinase inhibitor (Flavopiridol (HY-10005) analogue) that effectively inhibits HsGSK3β (IC50=59 nM), HsCDK9/CyclinT (IC50=64 nM), HsCDK5/p25 (IC50=1.093 µM) and HsCDK2/CyclinA (IC50=1.725 µM). CDK9/10/GSK3β-IN-1 has anti-cancer cellular activity comparable to or higher than that of Flavopiridol. CDK9/10/GSK3β-IN-1 shows high anti-proliferative activity in vitro against up to seven cancer cell lines[1].
Droxidopa-13C2,15N (hydrochloride) is deuterium labeled Droxidopa. Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); Droxidopa(L-DOPS) is capable of crossing the protective blood–brain barrier[1][2].