E3 ligase Ligand 1 is a Ligand for E3 Ligase extracted from patent WO/2017/030814A1 compound example 202, used in PROTAC technology.
ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. ERAP1-IN-1 competitively inhibits ERAP1 activity towards a nonamer peptide representative of physiological substrates[1].
PNU 37883 hydrochloride (PNU 37883A) is a selective vascular ATP-sensitive potassium (Kir6, KATP) channels blocker. PNU 37883 hydrochloride has diuretic effects with specific binding in kidney and vascular smooth muscle rather than in brain or pancreatic beta cells[1][2].
HT-2 Toxin is an active, deacetylated metabolite of the T-2 toxin. HT-2 toxin inhibits protein synthesis and cell proliferation in plants[1][2].
Umesolerbart (REGN5714) is a Bet v1 specific mAb. Umesolerbart (REGN5714)bind to homologous allergens in Alder, Hazel and hornbeam[1].
YL-109 is a novel anticancer agent which has ability to inhibit breast cancer cell growth and invasiveness in vitro and in vivo.IC50 value: 85.7 nM(MCF-7 cells proliferation) [1]Target: AhR signaling activcatorin vitro: YL-109 strongly inhibited cell proliferation of MCF-7 cells in a dose-dependent manner (IC50= 85.8 nM). Surprisingly, YL-109 had an anti-proliferative effect in a dose-dependent manner (IC50 = 4.02 μM) on MDA-MB-231 cells. YL-109 repressed the sphere-forming ability and the expression of stem cell markers in MDA-MB-231 mammosphere cultures. YL-109 increased the expression of carboxyl terminus of Hsp70-interacting protein (CHIP), which suppresses tumorigenic and metastatic potential of breast cancer cells by inhibiting the oncogenic pathway. YL-109 induced CHIP transcription because of the recruitment of the aryl hydrocarbon receptor (AhR) to upstream of CHIP gene in MDA-MB-231 cells. Consistently, the antitumor effects of YL-109 were depressed by CHIP or AhRknockdown in MDA-MB-231 cells [1].in vivo: Mice treated with vehicle showed significantly enlarged tumors, whereas mice treated with YL-109 showed attenuated tumor growth using MCF-7 cells. Interestingly, YL-109 also suppressed tumor growth in mice injected with MDA-MB-231 cells. Compared with the vehicle control, YL-109 significantly reduced lung metastasis [1].
BDP R6G maleimide is a borodipyrromethane fluorophore with absorption and emission wavelengths similar to those of R6G rhodamine. Sulfhydryl labelling is a common protein modification where the cysteine residues in the protein allow more site-specific labelling than the NHS ester of the amine group. BDP R6G maleimide is a thiol reactive dye that reacts with thiol groups to form thioester bonds[1].
H-His(Trt)-OH is a histidine derivative[1].
Antibacterial agent 30 demonstrates excellent in vitro activity against Xoo with EC50 value of 1.9 μg/mL.
Fmoc-L-Lys(Pentynoyl-DIM)-OH is a click chemistry reagent containing an azide. Fmoc-L-Lys(Pentynoyl-DIM)-OH can be used as a SPPS building block for the “helping hand” strategy for purification of highly insoluble peptides. Solubilizing residues are attached to the Lys side-chains using Click-chemistry. The solubilizing tag can be removed with 1M hydrazine or hydroxylamine solution[1].
Podophyllotoxin is a potent inhibitor of microtubule assembly and DNA topoisomerase II.IC50 Value:Target: Topoisomerase II; Microtubule/TubulinPodophyllotoxin, a kind of non-alkaloid toxin lignan extracted from the roots and rhizomes of Podophyllum plant, has been shown to inhibit the growth of various carcinoma cells. Podophyllotoxin is a natural product that inhibits the polymerization of tubulin and has served as a prototype for the development of diverse antitumor agents in clinical use.
MAL3-101 is a Hsc70 modulator that inhibits Hsp70 ATPase activity, exhibits antiproliferative activity in breast cancer cells SK-BR-3 with IC50 of 27 uM; also exhibits antimyeloma effects on MM cell lines in vitro and in vivo in a xenograft plasmacytoma model, as well as on primary tumor cells and bone marrow endothelial cells from myeloma patients.
Praeruptorin C is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin C is a calcium antagonist with pD2′ value of 5.7[1].
KRAS G12C inhibitor 31 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 1. KRAS G12C inhibitor 31 can be used for the research of cancer[1].
CC-99282 is a potent and orally active cereblon (CRBN) E3 ligase modulator (CELMoD). CC-99282 co-opts CRBN to induce potent and targeted degradation of Ikaros and Aiolos. CC-99282 can be used for researching non-Hodgkin lymphomas[1].
Yohimbic acid hydrate is an amphoteric demethylated derivative of Yohimbine (HY-12715). Yohimbic acid hydrate exhibits vasodilatory action. Yohimbic acid hydrate also can be used for the research of osteoarthritis (OA)[1][2][3].
GZ-793A is an orally active and selective vesicular monoamine transporter-2 (VMAT2) inhibitor, with an Ki of 0.029 µM. GZ-793A inhibits the neurochemical effects of methamphetamine (METH)-induced dopamine release. GZ-793A can be used for research of METH addiction[1][2][3].
BAY-320 is a Bub1 inhibitor, with an IC50 of 680 nM for human Bub1 in the presence of 2 mM ATP.
Anagliptin is a highly selective, potent inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8/9 (IC50, 68, 60 nM, respectively).
OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells[1]. OTS514 hydrochloride induces cell cycle arrest and apoptosis[2].
PROTAC BRD9 Degrader-2 is a BRD9 bifunctional degrader for treating cancer.
1,7-Diphenyl-4-hepten-3-one, isolated from Alpinia officinarum, possess bioactivities against some pests, such as T. castaneum[1].
L-Homopropargylglycine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(S)-NADH-d1 is the deuterium labeled (S)-NADH. NADH is an orally active reduced coenzyme. NADH is a donor of ADP-ribose units in ADP-ribosylaton reactions and a precursor of cyclic ADP-ribose. NADH plays a role as a regenerative electron donor in cellular energy metabolism, including glycolysis, β-oxidation and the tricarboxylic acid (TCA) cycle[1][2].
Cefdinir (Omnicef) is a semi-synthetic, broad-spectrum antibiotic, which is proved to be effective for common bacterial infections of the ear, sinus, throat, and skin.Target: AntibacterialCefdinir is a third generation oral cephalosporin antibiotic. Cefdinir (Omnicef) is a semi-synthetic, broad-spectrum antibiotic in the third generation of the cephalosporin class, which is proved to be effective for common bacterial infections of the ear, sinus, throat, and skin. It can be used to treat infections caused by several Gram-negative and Gram-positive bacteria. It is available in US as Omnicef by Abbott Laboratories and in India as Cednir by Abbott, Kefnir by Glenmark and Cefdiel by Ranbaxy. As of 2008, cefdinir was the highest-selling cephalosporin antibiotic in the United States, with more than US$585 million in retail sales of its generic versions alone.Cefdinir, a new oral 2-amino-5-thiazolyl cephalosporin, inhibited the luminol-amplified chemiluminescence (LACL) response of human neutrophils stimulated by PMA but not opsonized zymosan, in a concentration-dependent but not time-dependent manner. The LACL response to opsonized zymosan in cytochalasin B-treated neutrophils was, however, inhibited by cefdinir. Furthermore, cefdinir inhibited LACL generation in cell-free systems consisting of H2O2, NaI, and either horseradish peroxidase or a myeloperoxidase-containing neutrophil extract. Orthodianisidine oxidation in these two acellular systems was inhibited by cefdinir.
SRT 1720 dihydrochloride is a selective and orally active activator of SIRT1 with an EC50 of 0.10 μM, and shows less potent activities on SIRT2 and SIRT3[1].
Elebsiran is an antiviral agent[1].
Gomisin O is isolated from the fruits of Schizandra chinensis[1].
Y-27632 dihydrochloride is a cell-permeable, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively.
Mal-PEG4-C2-NH2 TFA is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].