MNK1/2-IN-5 is a potent and selective MNK1/2 inhibitor as a therapeutic agent.
Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.
Streptozocin is a potent DNA-methylating agent, with IC50s of 11.7, 904 and 1024 μg/mL in HL60, K562 and C1498 cells respectively.
VAL-083 is an alkylating agent that creates N7 methylation on DNA, with antitumor activity.
Rehmapicrogenin, isolated from the root of Rehmannia glutinosa, exhibits potent anti-inflammatory effect by inhibiting iNOS, COX-2 and IL-6[1].
Volixibat (SHP626) is a highly selective, minimally absorbed, and competitive apical sodium-dependent bile acid transporter (ASBT) inhibitor. Volixibat has potential for treatment for non-alcoholic steatohepatitis (NASH)[1][2].
AZD8542 is an antagonist of Smoothened (SMO) with potential as an oncology therapeutic.
Umirolimus, a macrocyclic triene lactone Rapamycin derivative, is powerful immunosuppressant and anti-inflammatory agent. Umirolimus has highly lipophilicity and can be used drug-eluting stent (DES) applications[1].
Boc-Gln-Gly-Arg-AMC is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development[1].
Etidronic acid is a bisphosphonate used in detergents, water treatment, cosmetics and pharmaceutical treatment.Target: OthersEtidronic Acid is a chelating agent and may be added to bind to or counter the effects of substances such as arsenic, iron, or other metal ions that can occur in the presence of some soaps. Etidronic acid also acts to retard oxidation of fatty acids. For clarification, a chelator, or chelating agent is a binding component added to many cosmetics, beauty products, and water softeners to form multiple bonds with a single metal ion and neutralize it.
Leupeptin Ac-LL is a protease inhibitor from actinomycetes. Leupeptin Ac-LL has antiplasmin activity[1].
L-Valyl-L-phenylalanine (Valylphenylalanine; H-VAL-PHE-OH) has been reported as biocompatible polymer.
Rucaparib (AG014699) tartrate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].
Pde7-in-3 (example 2) is an inhibitor of the phosphodiesterase PDE7 with potential analgesic activity. PDE7-IN-3 can be used to study inflammatory, neuropathic, visceral and nociceptive pain[1].
Kasugamycin is an important amino-glycoside family antibiotic and widely used for veterinary and agricultural applications.
Venadaparib (IDX-1197) hydrochloride is a potent and selective PARP inhibitor with anticancer activities. Venadaparib hydrochloride can be used for solid tumors research[1][2].
JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models[1].
Pimecrolimus hydrate (SDZ-ASM 981 hydrate) is a potent, nonsteroid and orally active calcineurin inhibitor. Pimecrolimus hydrate shows anti-inflammatory activity. Pimecrolimus hydrate has the potential for the research of atopic dermatitis and oral erosive lichen planus[1][2][3].
LY 178002 is a potent inhibitor of 5-lipoxygenase, phospholipase A2, with IC50 of 0.6 μM for 5-1ipoxygenase, inhibits cellular production of LTB4 by human polymorphonuclear leukocytes, and shows relatively weak inhibition on cyclooxygenase.
Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
Enalapril D5 maleate is deuterium labeled Enalapril, which is an angiotensin converting enzyme (ACE) inhibitor.
CKLF1-C19 is the C-terminal peptide of human chemokine-like factor 1 (CKLF1). CKLF1-C19 interacts with CCR4, and inhibits chemotaxis induced by both CKLF1 and CCL17. CKLF1-C19 can suppress allergic lung inflammation via inhibiting chemotaxis mediated by CCR3 and CCR4[1].
1,3-Diphenylurea-d10 is the deuterium labeled 1,3-Diphenylurea[1].
1H-Benzotriazole-4,5,6,7-d4 is the deuterium labeled 1H-Benzo[d][1,2,3]triazole[1].
H-DL-Glu(Ome)-OH is a glutamic acid derivative[1].
Tetraethyl heptane-1,7-diylbis(phosphonate) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
GS-626510 is a potent, and orally bioavailable BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively[1].
JNJ-64264681 is a potent, orally active, selective and irreversible covalent BTK inhibitor. JNJ-64264681 exhibits good pharmacokinetic characteristics and can be used for cancer and autoimmune diseases research[1].
LEI110 (LEI-110) is a potent Phospholipase A2 group XVI (PLA2G16) inhibitor with Ki of 20 nM, also has activity on HRASLS2, RARRES3 and iNAT (pIC50=6.8-7.6); reduces cellular arachidonic acid levels and oleic acid-induced lipolysis in human HepG2 cells; LEI110 is a selective pan-inhibitor of the HRASLS-family of thiol hydrolases (i.e. PLA2G16, HRASLS2, RARRES3 and iNAT).
Cys-McMMAF is the released payload of AlMcMMAF, an anti-5T4 humanized A1 antibody conjugated to the microtubule disrupting MMAF (HY-15579) via a maleimidocaproyl linker. Cys-McMMAF has antitumor efficacy in two tumor mouse models (H1975 and MDA-MB-361-DYT2 models)[1].