4α-Methylcholesterol is a Cholesterol derivative. 4α-Methylcholesterol can oxidize 3-hydroxy steroid, with the apparent Km of 12.6 μM[1][2].
(9Z,12E)-Tetradecadien-1-yl acetate is the main component of pheromone of insects Ephestia Kuehniella and Plodia Interpunctella, and cereal pests[1].
SREBP/SCAP-IN-2(compound 13) is a selectiveSREBP/SCAPinhibitor[1].
p-Anisic acid (4-Methoxybenzoic acid) is one of the isomers of anisic acid, with anti-bacterial and antiseptic properties[1].
Werner syndrome RecQ helicase-IN-2 (example 57) is a potent Werner syndrome RecQ DNA helicase enzyme (WRN) inhibitor and can be used in cancer research[1].
Cyclo(Arg-Gly-Asp-D-Phe-Val) is an integrin αvβ3 inhibitor. Cyclo(Arg-Gly-Asp-D-Phe-Val) has antitumor activity. Cyclo(Arg-Gly-Asp-D-Phe-Val) can be used for the research of acute myeloid leukemia[1].
D-(+)-Sorbose, an active enantiomer of D-Sorbose, which inhibits disaccharidase activity and demonstrates suppressive action on postprandial blood levels of glucose and insulin in the rat. D-sorbose acts as a sweetener may contribute to the prevention of lifestyle-related diseases, such as type 2 diabetes mellitus[1].
N-Tetradecanoyl-DL-homoserine lactone is a serine derivative[1].
Voriconazole (UK-109496) camphorsulfonate is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole camphorsulfonate exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes[1][2].
SynB1 is a cell penetrating polypeptide, internalized by, or is associated with lipid vesicle (LV). SynB1 can be used to lipid vesicle-mediated delivery to cells[1].
(R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs[1][2].
Thalidomide-NH-C9-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-NH-C9-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs[1].
Cathepsin X-IN-1 (compound 25) is a potent Cathepsin X inhibitor with an IC50 of 7.13 µM. Cathepsin X-IN-1 decreases PC-3 cell migration with low cytotoxic[1].
PU-141 is a potent, selective CBP/p300 inhibitor that inhibits SK-N-SH cell growth with GI50 of 0.48 uM; blocks growth of SK-N-SH neuroblastoma xenografts in mice, also reduces histone lysine acetylation in vivo at concentrations that block neoplastic xenograft growth.
Adenosine-3′-13C is the 13C labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiolo
Filorexant (MK-6096) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding).
LSP-GR3 is a novel chemically-modified RNA oligonucleotides, called splice modulating oligomers (SMOs), which potently and specifically modulate GluR alternative splicing to GluR3-flip expression throughout the CNS.
Tenovin-3 is able to increase p53 levels, determined in MCF-7 cells treated for 6 hr at 10 μM.Target: p53in vitro: Tenovins inhibit the activities of human SirT1 and SirT2, two members of the NAD+-dependent class III histone deacetylases that also belong to the sirtuin family.[1]
Iriflophenone 3-C-β-D-glucopyranoside, isolated from Cyclopia genistoides, has antioxidant activity[1].
PI3Kγ inhibitor 6 (compound 9) is a PI3Kγ inhibitor. PI3Kγ inhibitor 6 can be used for the research of inflammatory and autoimmune diseases[1].
3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells[2]. 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity[2].
PXS-5153A is a potent, selective, orally active and fast-acting inhibitor of lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3), with an IC50 of <40 nM for LOXL2 across all mammalian species and an IC50 of 63 nM for human LOXL3. PXS-5153A could reduce crosslinks and ameliorates fibrosis.
KPT-330, analog of KPT-185, is an orally bioavailable selective CRM1 inhibitor.IC50 value: Target: CRM1in vitro: As the clinical candidate analog of KPT-185, KPT-330 exhibits similar effects on the viability of T-ALL cells and elicits rapid apoptotic response. KPT-330 also reduces cell growth in MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3, and DND-41 cell lines, with IC50 values of 34-203 nM [1]. in vivo: KPT-330 dramatically suppresses the growth of T-ALL cells (MOLT-4) and AML cells (MV4–11) in vivo, with little toxicity to normal haematopoietic cells [1]. In SCID mice with diffuse human MM bone lesions, KPT-330 inhibits MM-induced bone lysis and prolongs survival. Moreover, KPT-330 directly impairs osteoclastogenesis and bone resorption by blocking RANKL-induced NF-κB and NFATc1, with minimal impact on osteoblasts and BMSCs [2].
Atractylochromene is a potent dual inhibitor of 5-LOX/COX-1 with IC50s of 0.6 and 3.3 μM, respectively[1].
Glaucogenin C mono-D-thevetoside can be isolated from the roots of Cynanchum stauntonii[1].
Filgotinib (maleate) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM and 116 nM for JAK1, JAK2, JAK3 and TYK2, respectively. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research[1][2].
ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC50s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects[1][2].
Endoproteinase Asp-N (Asp-N) is a metalloprotease that can specifically cleave the N-terminal side of aspartyl and cysteic acid residues[1].
JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain[1].
Ropinirole-d3 (hydrochloride) is the deuterium labeled Ropinirole hydrochloride[1]. Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease[2][3].