Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
UMB68 sodium is a selective GHB receptor ligand. UMB68 sodium displaces [3H]NCS-382 with an IC50 of 38 nM in rat cerebrocortical membranes. UMB68 sodium has no significant affinity at GABAB receptors, cannot be metabolized to GABA-active compounds[1].
ERK-CLIPTAC is a PROTAC molecule that triggers the degradation of ERK[1].
SU16f is a potent and selective PDGFRβ inhibitor with IC50s of 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively[1]. Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs (gastric cancer-derived mesenchymal stem cells) conditioned medium in gastric cancer cell proliferation and migration[2].
PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit[1].
Lachnone A is a chromone derivative isolated from the filamentous fungus Lachnum sp. BCC 2424[1].
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer[1].
1-Bromo-4-(trifluoromethyl)benzene-d4 is the deuterium labeled 1-Bromo-4-(trifluoromethyl)benzene[1].
BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8.
N6-(2-Phenylethyl)adenosine is a selective A1 adenosine receptor agonist.
Euphorbiasteroid is a tricyclic diperpene of Euphorbia lathyris L., inhibits tyrosinase, and increases the phosphorylation of AMPK, with anti-cancer, anti-virus, anti-obesity and multidrug resistance-modulating effect[1].
L-796449 is a potent PPARγ agonist. L-796449 shows neuroprotective. L-796449 has the potential for the research of stroke[1].
FLT3-IN-15 is a highly potent and orally active FLT3 inhibitor with IC50s of 0.87 nM and 0.32 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-15 can be used for researching acute myeloid leukemia[1].
TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC50 of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors[1].
5-Carboxymethyluridine is a thymidine analogue. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively hypotension. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 can be used for hypotension study[1].
Ibutamoren (Mesylate) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist.
m-PEG2-Ms is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
N-(Biotin-PEG4)-N-bis(PEG4-Boc) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
SB-200646 is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646 is orally active and has electrophysiological and anxiolytic properties in vivo[1][2].
Hypoxanthine-13C,15N2 is a 15N-labeled and 13C-labled Furaltadone. Furaltadone, a nitrofuran drug, has the potential for the study in infections of chickens with salmonella enteritidis. Furaltadone is inhibitory and bactericidal in vitro for staphylococci
CP-24879 (hydrochloride) is a potent, selective and combined delta5D/delta6D inhibitor. CP-24879 (hydrochloride) can significantly reduce intracellular lipid accumulation and inflammatory injury in hepatocytes. CP-24879 (hydrochloride) exhibits superior antisteatotic and anti-inflammatory actions in fat-1 and ω-3-treated hepatocytes, and can be used for non-alcoholic steatohepatitis research[1][2].
Ethyl 2-amino-3-(4-hydroxyphenyl)-2-methylpropanoate is a tyrosine derivative[1].
Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. Cathepsin K inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78)[1].
6,7-Diaminoquinoxaline-2,3-dione dihydrochloride is a fluorescent dye that reacts with aldehydes[1].
Isovanillin is an aldehyde oxidase inhibitor[1]. Antispasmodic activities[2]. Antidiarrheal activities[3].
TAT-GluA2 3Y is an inhibitor of AMPA receptor endocytosis. TAT-GluA2 3Y induces increased hind paw withdrawal latencies following thermal and mechanical stimuli in rats. TAT-GluA2 3Y also exhibits antinociceptive effects in a rat model of neuropathic pain. TAT-GluA2 3Y rescues pentobarbital-induced memory retrieval deficits in a rat model of learning and memory.
Ipomoeassin F is a potent and selective endoplasmic reticulum (ER) protein-translocation inhibitor by targeting the pore-forming subunit of the Sec61 complex (Sec61α) at the ER membrane. Ipomoeassin F selectively inhibits the ER membrane translocation of SARS-CoV-2 proteins. Ipomoeassin F block the ER translocation of secretory proteins and type I transmembrane proteins (TMPs), but not type III TMPs[1][2][3].
Haloprogin is a potent antifungal agent. Haloprogin has activity against dermatophytes, Candida spp and a limited number of Gram-positive bacteria[1].
Ifenprodil tartrate is a novel N-methyl-D-aspartate (NMDA) receptor antagonist that selectively inhibits receptors containing the NR2B subunit.