MRTX-1257 is a selective, irreversible, covalent and oral active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells[1].
Methyl 2-amino-3,3,3-trifluoropropanoate hydrochloride is an alanine derivative[1].
Anti-osteoporosis agent-2 (Compound 10) is an anti-osteoporosis agent. Anti-osteoporosis agent-2 inhibits differentiation on osteoclast induced by RANKL[1].
Lipid X is a novel monosaccharide precursor of Lipid A (the active moiety of gram-negative endotoxin). Lipid X is protective against endotoxin administered to mice and sheep and against life-threatening gram-negative infections in mice[1].
Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist[1]. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone[2]. Anti-inflammatory agent.
Glycolic acid oxidase inhibitor 1 is a glycolate oxidase inhibitor, extracted from patent EP0021228A1, in Table IV.
RITA is an inhibitor of p53-HDM-2 interaction, binds to p53dN, with a Kd of 1.5 nM, and also induces DNA-DNA cross-links.
(R)-(+)-Dimethindene maleate is an orally active H1-receptor blocker with antihistaminic properties in pigs[1].
Cathepsin D and E FRET Substrate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D[1].
IDO1/TDO-IN-6 (compound 11) is a dual inhibitor of IDO1/TDO with IC50s of 2.25 and 2.89 μM, respectively. IDO1/TDO-IN-6 has inhibitory effects on IDO1 and TDO, with Ki values of 1.9 and 3.1 μM, respectively. IDO1/TDO-IN-6 can be used in cancer and immunology research[1].
SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active dopamine D1/D5 receptor antagonist[1]. SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM and attenuates cocaine effects in vivo[2].
Methionine-d3 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
Taxacin is a natural product, that can be isolated from seeds of Yew[1].
Tetradecyltrimethylammonium-d38 (bromide) is the deuterium labeled Tetradecyltrimethylammonium (bromide)[1]. Tetradecyltrimethylammonium bromide, an organic building block, is a cationic surfactant with asymmetrical structure[2][3].
MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA)[1].
Indoramin is an orally active antihypertensive agent. Indoramin is also selective for the α1A-adrenoceptor[1].
gp120-IN-2 (compound 4i) is a potent HIV-1 gp120 inhibitor with an IC50 of 7.5 µM and CC50 of 112.93 µM. gp120-IN-2 shows anti-HIV-1 activity. gp120-IN-2 shows cytotoxicity in a dose dependent manner in SUP-T1 cells[1].
E1R is a positive allosteric modulator of sigma-1 receptors with cognition-enhancing activity[1].
7-Hydroxycoumarin-3-carboxylic acid N-succinimidyl ester is the amine-reactive succinimidyl ester of 7-Hydroxycoumarin-3-carboxylic acid. 7-Hydroxycoumarin-3-carboxylic acid N-succinimidyl ester is a blue fluorescent dye for labeling proteins and nucleic acids[1].
Interferon receptor agonist is an interferon (IFN) receptor agonist.
Zndm19 is a New Delhi Metallo-β-lactamase-1 (NDM-1) inhibitor. Zndm19 can be used for the research of drug-resistant bacterial infections[1].
MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. Anticancer activities[1][2].
Feralolide is a dihydroisocoumarin isolated from the methanolic extract of aloe vera resin. Feralolide is also a dual inhibitor of AChE and BuChE, with IC50s of 55 μg/mL and 52 μg/mL respectively. Feralolide has antioxidant activity and inhibits 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2, 2′-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS). Feralolide could be used in research into cognitive disorders such as Alzheimer's disease, potentially restoring and enhancing memory[1].
Bisandrographolide A (BAA) activates TRPV4 channel with an EC50 of 790-950 nM. Bisandrographolide A can bind to CD81 and suppress its function. Bisandrographolide A is an anti-inflammatory, immunostimulant, and antihypertensive compound[1][2].
Astegolimab (MSTT 1041A; RG 6149) is a human IgG2 monoclonal antibody that blocks IL-33 signaling by targeting ST2, the IL-33 receptor. Astegolimab has the potential for chronic obstructive pulmonary disease (COPD) research[1].
Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity[1].
Biotin-PEG6-alcohol is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Telmesteine is an amucolitic agent. Telmesteine has anti-protease activity. Telmesteine inhibits LPS-induced NO production in RAW264.7 cells. Telmesteine can be used for research of inflammation, such as acute and chronic bronchitis and obstructive airways disease[1][2].
Penicillin V Potassium is an antibiotic useful for the treatment of a number of bacterial infections, is a penicillin that is orally active, acts by inhibiting the biosynthesis of cell-wall peptidoglycan.
G43-C3-TEG is a glycosyl-transferase inhibitor. G43-C3-TEG reduces the biofilm formation by decreasing the production of EPS (extracellular polysaccharides)[1].