T7942

Tranylcypromine hemisulfate (Tranylcypromine Sulfate) is an inhibitor of monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1) with a rapid onset of activity.

FLT3-IN-22 (compound 22f) is a potent FLT3 inhibitor with IC50 values of 0.941 nM for FLT3 and 0.199 nM for the FLT3/D835Y mutant. It demonstrates significant antiproliferative effects against MV4-11 cells and Ba/F3 cell lines expressing mutant FLT kinase variants, including FLT-D835Y and FLT3-F691L [1].

DCLK1-IN-2 (Compound I-5) is a potent inhibitor of DCLK1, exhibiting an IC50 of 171.3 nM, and demonstrates significant antiproliferative effects on SW1990 cell lines with an IC50 of 0.6 μM, as well as in vivo antitumor potency [1].

BuChE-IN-8 (compound 19c), a butyrylcholinesterase (BuChE) inhibitor, exhibits an IC50 value of 559 nM and concurrently inhibits human β-secretase (BACE1) and Aβ40 aggregation. It also demonstrates notable antiamnesic properties [1].

BuChE-IN-9 (compound 22a), an eqBuChE (equine serum-derived butyrylcholinesterase) inhibitor, exhibits potent activity with an IC50 of 173 nM. In addition to eqBuChE, it also inhibits human BACE1, Aβ aggregation, and mouse GABA transporters 1 and 4 (mGAT1 and mGAT4). Notably, BuChE-IN-9 demonstrates significant antiamnesic properties [1].

Compound 8, a cholic acid derivative, functions as a selective TGR5 agonist and exhibits an EC50 value of 5 μM [1].

TGR5 agonist 4 (compound 19), a cholic acid derivative, selectively activates the TGR5 receptor with an EC50 of 4 μM [1].

SARS-CoV-2-IN-61 (compound 8i) is a potent SARS-CoV-2 PLpro inhibitor, with an IC50 of 16 µM, and exhibits antiviral activities [1].

LM-41 is a TEAD-binding agent with potential anticancer activity that strongly reduces the expression of CTGF, Cyr61, Axl and NF2, and can be used in the study of breast cancer.

AF-2112, a TEAD inhibitor derived from Flufenamic acid, significantly diminishes the expression of CTGF, Cyr61, Axl, and NF2.

Tubulin Polymerization-IN-50 (compound 7n) serves as an inhibitor of tubulin polymerization, exhibiting an IC50 of 5.05 μM in SK-Mel-28 cells and inducing cell cycle arrest at the G2/M phase [1].