Fmoc-N-amido-PEG20-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Viteralone (compound 5) is a natural product that can be isolated from Vitex negundo. Viteralone is cytotoxic to HL-60 cancer cells[1].
Nav1.8-IN-4 (compound 9a) is a Nav1.8 channel inhibitor (IC50=0.014 μM). Nav1.8-IN-4 can be used for research on pain-related diseases[1].
Chlorahololide D is a potent and selective Potassium Channel blocker with an IC50 value of 2.7 µM. Chlorahololide D is a nature product that could be isolated from the whole plant of Chloranthus holostegius[1].
FEMA 4809 is a TRPM8 receptor agonist (EC50=0.2 nM) for use as a cooling agent. TRPM8 is the ion channel responsible for the cool perception[1].
7-Methoxyisoflavone is an isoflavone derivative and also an activator of adenosine monophosphate-activated protein kinase (AMPK).
H-alpha-Prg-D-Ala-OH is a click chemistry reagent containing an azide group[1].
Smurf1-IN-1 is an orally active and selective inhibitor of specific E3 ubiquitin protein ligase 1 (SMURF1) with an IC50 of 92 nM. Smurf1-IN-1 has significant efficacy in rats model of pulmonary hypertension[1].
Eupalinolide A, isolated from Eupatorium lindleyanum, induces the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90[1].
Tau Peptide (275-305) (Repeat 2 domain) is the Alzheimer's tau fragment R2, corresponding to the second repeat unit of the microtubule-binding domain, which is believed to be pivotal to the biochemical properties of full tau protein[1].
3-Bromo-7-nitroindazole is a more potent and selective inhibitor of neuronal nitric oxide synthase (nNOS) than eNOS or inducible nitric oxide synthase (iNOS). 3-Bromo-7-nitroindazole affects the intercellular messenger nitric oxide (NO) synthesis throughout the body and brain[1].
JF646, Tetrazine, a red fluorescent dye, is supplied with a tetrazine reactive handle for copper-free click chemistry. JF646, Tetrazine is suitable for confocal fluorescent imaging, super-resolution microscopy (SRM) techniques such as dSTORM (live and fixed cells) and STED imaging. JF646, Tetrazine is also suitable for flow cytometry.
Brexpiprazole-d8-1 is the deuterium labeled Brexpiprazole[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic drug, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[2][3].
Lexanersen (WVE-120102) is an antisense oligonucleotide used for the study of Huntington's disease[1].
Isorhynchophylline (IRN), an alkaloid isolated from Uncaria rhynchophylla, possesses the effects of lowered blood pressure, vasodilatation and protection against ischemia-induced neuronal damage.IC50 value:Target:In vitro: Isorhynchophylline concentration-dependently inhibited the platelet-derived growth factor (PDGF)-BB-induced proliferation of PASMCs. Fluorescence-activated cell-sorting analysis showed that isorhynchophylline caused G0/G1 phase cell cycle arrest [2]. Isorhynchophylline can significantly attenuate the cardiomyocyte hypertrophy induced by AngⅡ [3].In vivo: Isorhynchophylline significantly improved spatial learning and memory function in the D-gal-treated mice. Isorhynchophylline significantly increased the level of glutathione (GSH) and the activities of superoxide dismutase (SOD) and catalase (CAT), while decreased the level of malondialdehyde (MDA) in the brain tissues of the D-gal-treated mice [1]. Isorhynchophylline prevented monocrotaline induced pulmonary arterial hypertension in rats, as assessed by right ventricular (RV) pressure, the weight ratio of RV to (left ventricular+septum) and RV hypertrophy. Isorhynchophylline significantly attenuated the percentage of fully muscularized small arterioles, the medial wall thickness, and the expression of smooth muscle α-actin (α-SMA) and proliferating cell nuclear antigen (PCNA) [2].
Endo-β-N-acetylglucosaminidase (Endo A) is an Endo-β-N-acetylglucosaminidases (ENGases) from Arthrobacter protophormiae. Endo-A can transfer a high-mannose type oligosaccharide to monosaccharides such as N-acetylglucosamine (GlcNAc) and glucose to form a new oligosaccharide. Endo-A catalyzes glycopeptide synthesis by using Man3GlcNAc-oxazoline[1].
Vinaginsenoside R4, isolated from the leaves of hydroponic Panax ginseng. It has an inhibitory effect on melanin biosynthesis without any cytotoxic effects on the melan-a cells, and enhances the depigmentation on the zebrafish[1].
PROTAC GPX4 degrader-1 (DC-2) is a PROTAC-based GPX4 degrader, with a DC50 of 0.03 μM in HT1080 cells[1].
Griffipavixanthone can be extracted from Garcinia schomburgkiana. Griffipavixanthone induces cell apoptosis through mitochondrial apoptotic pathway accompanying with ROS production. Griffipavixanthone is an anti-cancer agent. Griffipavixanthone is a weak sucrase inhibitor (IC50: 4.58 mM)[1][2][3].
α-Chaconine, isolated from a Solanum tuberosum L. cv Jayoung, inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects[1].
Apolizumab (Hu1D10) is a humanized monoclonal anti-Human leukocyte antigen-DR beta-chain antibody. Apolizumab can mediate apoptosis of chronic lymphocytic leukemia (CLL) cells in vitro[1][2].
Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively)[1]. Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model[2].
PIPES-d18 is the deuterium labeled PIPES[1]. PIPES (1,4-Piperazinediethanesulfonic acid) is an important component of PIPES buffer agent used in biochemistry[2].
Sortin2 is a synthetic compound. Sortin2 can affect protein targeting to the vacuole in Saccharomyces cerevisiae[1].
Dimethylnitrosamine (NDMA) is a potent hepatotoxin, carcinogen and mutagen. Dimethylnitrosamine can be used to induces liver tumors[1][2].
Gastrazole (JB95008) is potent and selective CCK2/gastrin receptor antagonist. Gastrazole can decrease the level of gastric acid. Gastrazole inhibits the Gastrin-stimulated growth of pancreatic cancer[1][2].
Anticonvulsant agent 1 is an anticonvulsant agent extracted from patent WO2001062726A2, Compound 156.
Olopatadine-d3 hydrochloride (ALO4943A-d3) is the deuterium labeled Olopatadine hydrochloride. Olopatadine hydrochloride (ALO4943A) is a histamine blocker used to treat allergic conjunctivitis[1][2].
Phytochelatin 5 is metal-binding compound produced by plants. Phytochelatin 5 may reduce bioavailability of dietary toxic metals such as cadmium[1].
HSV-1/HSV-2-IN-1 (compound 7d) is a HSV-1 and HSV-2 inhibitor, with EC50s of 7.6, 7.6, 4, and 12 μM for HSV-1 (KOS), HSV-2 (G), HSV-1 TK- KOS ACVr and vaccinia virus in human embryonic lung fibroblast cell cultures[1].