NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease[1].
Anticancer agent 121, an inhibitor of human lactate dehydrogenase A enzyme (hLDHA), has good anticancer activities and can be used for anticancer research[1].
FR-229934 is a PDE V inhibitor extracted from patent WO2019130052A1. FR-229934 can be used for the research of pulmonary arterial hypertension and erectile dysfunction[1].
Hippuryl-His-Leu-OH is a substrate for detecting the activity of angiotensin I converting enzyme. The His-Leu released by Hippuryl-His-Leu-OH can react with o-phtbaldialdehyde or Fluorescamine (HY-D0715) for fluorescence detection[1][2][3].
CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2].
Norbraylin, a natural prenylated coumarin, is a PDE4D2 inhibitor with an IC50 value of 7.15 μM[1].
(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD)[1]. (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM[2].
TMP780 is an inverse agonist of RORγt with an IC50 of 13 nM. RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders[1].
Dihydrolanosterol-d7 is deuterium labeled Dihydrolanosterol. Dihydrolanosterol is a subtrate of CYP51 and a cholesterol biosynthesis inhibitor[1].
6-Methoxytricin (Compound 6) is an flavonoid isolated from Artemisia iwayomogi. 6-Methoxytricin (Compound 6) is an inhibitor on aldose reductase (AR) and advanced glycation endproduct (AGE) formation activities with IC50 values of 30.29 μM and 134.88 μM, respectively. 6-Methoxytricin (Compound 6) has potential as an anti-diabetic complications agent[1].
Ginkgolic Acid is a natural compound with suspected cytotoxic, allergenic, mutagenic and carcinogenic properties, and it can inhibit protein SUMOylation both in vitro and in vivo without affecting in vivo ubiquitination.
4,5-Dimethoxycanthin-6-one is a potent and uncompetitive inhibitor of CYP1A2-mediated phenacetin O-deethylation with an IC50 value of 1.7μM and a Ki value of 2.6 μM. 4,5-Dimethoxycanthin-6-one, as an alkaloid, is isolated from the wood of Picrasma quassioides BENNET (Simaroubaceae)[1][2].
PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor.
FASN-IN-5 (example 11), a FASN inhibitor, can be used for the research of TH17- or CSF1 -mediated disease or disorder such as cancer, immunological disorders, and obesity[1].
hCAII-IN-2 (Compound 11f) is a cytosolic human carbonic anhydrase (hCA) inhibitor with Ki values of 261.4, 3.8, 19.6 and 45.2 nM against hCA I, hCA II, hCA IX and hCA XII, respectively[1].
Apixaban 13CD3 (BMS-562247-01 13CD3) is a deuterium labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].
(Rac)-Sitagliptin-d4((Rac)-MK-0431-d4) hydrochloride is a labelled racemic Sitagliptin. Sitagliptin (MK-0431) hydrochloride is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[1].
Viscumneoside III, a dihydroflavone O-glycoside, is a potent tyrosinase inhibitor with an IC50 of 0.5 mM. Viscumneoside III has anti-angina pectoris[1].
MMP2-IN-1 is a moderate potenet MMP2 inhibitor with IC50 of 6.8 µM. MMP2-IN-1 exhibits remarkable antiproliferative activity in certain cancer cells by arresting the cell cycle and inducing apoptosis[1].
Palmitic acid-d4-1 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2][3].
ALDH3A1 inhibitor EN40 is a potent and selective, covalent, in vivo-active inhibitor of ALDH3A1 with IC50 of 2 uM, demonstrates no activity against ALDH1A3 and ALDH6A1 at 30 uM; also does not show any observable competition against lysine-reactive probe labeling of A549 proteomes; specifically inhibits the lung cancer cell lines expressing ALDH3A1, but not in the cell lines that do not express ALDH3A1, inhibits ALDH3A1 activity and impairs lung cancer pathogenicity in vivo.
γ-Glu-Tyr, a competitive inhibitor of dipeptidyl peptidase-IV (DPP-IV) (IC50=6.77 mM), is a potentially functional component of the type 2 diabetes diet[1].
TLK117, the active metabolite of TLK199, selective inhibits Glutathione S-transferase P1–1 (GSTP1-1) with a Ki of 0.4 μM for GSTP. TLK117 also competitively inhibits glyoxalase I with a Ki of 0.56 μM.
BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer[1][2][3].
Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt is a MMP12 substrate, and can be used to detect MMP12 enzyme activity[1].
Aderamastat (FP-025) is an orally active matrix metalloproteinase 12 (MMP-12) inhibitor. Aderamastat can be used for the research of asthma, chronic obstructive pulmonary disease (COPD), and pulmonary fibrosis[1].
Cbl-b-IN-3 (Compound 23) is a casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) inhibitor with an IC50 of < 1 nM. Cbl-b is an E3 ubiquitin ligase that negatively regulates T-cell activation[1].
Isopedicin potently and concentration-dependently inhibits superoxide anion (O2 U?) production in formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP)-activated cells. Isopedicin increases cAMP formation and PKA activity in FMLP-activated cells by inhibiting phosphodiesterase (PDE) activity[1].
MY33-3 is a small-molecule inhibitor of RPTPβ/ζ (PTPRZ1) with IC50 of 0.1 uM, significantly increases the phosphorylation of key tyrosine residues of RPTPβ/ζ substrates involved in neuronal survival and differentiation; blocks ethanol conditioned place preference, shows limited effects on ethanol-induced ataxia, and potentiates the sedative effects of ethanol in mice; increases levels of phosphorylated ALK and TrkA in neuroblastoma cells, modulates signaling pathways activated by alcohol.
Ganoderic acid GS-1, a highly oxygenated lanostane-type triterpenoid, has anti-HIV-1 protease activities with an IC50 of 58 μM[1].