T7300

GDC-0575 (ARRY-575) is a highly-selective oral small-molecule Chk1 inhibitor(IC50 of 1.2 nM).

PARP10-IN-2 is a potent inhibitor of PARP10, a mono-ADP-ribosyltransferase, with an IC50 value of 3.64 μM for human PARP10. It also inhibits PARP2 and PARP15, with IC50 values of 27 μM and 11 μM, respectively.

SIRT2-IN-11 is a potent and selective SIRT2 inhibitor (IC50 = 12 nM). It increases tubulin acetylation without affecting SIRT1/3, used for studying SIRT2 function in cancer and neuroprotection.

eIF4A3-IN-9, a silvestrol analogue, disrupts the assembly of the eIF4F translation complex, exhibiting EC50 values of 29, 450, and 80 nM for myc-LUC, tub-LUC, and growth inhibition in MBA-MB-231 cells, respectively. It is utilized in researching human cancer pathogenesis [1].

METTL3-IN-2, a potent METTL3 inhibitor, exhibits an IC50 value of 6.1 nM, effectively impairing the proliferation of Caov3 cancer cells.

PF-07054894 is a potent antagonist of the CCR6 and a targeted G protein-coupled receptor (GPCR), useful in the research of inflammatory bowel disease.

cis-ccc_R08 infection . cis-ccc_R08 is a cccDNA (covalently closed circular DNA) inhibitor .

PCSK9-IN-13 (compound 3f) is a potent PCSK9 inhibitor with an IC50 of 537 nM. It antagonizes the binding of the low-density lipoprotein receptor (LDLR) to PCSK9 by interacting with a cryptic binding groove on the PCSK9 protein. Since PCSK9 normally mediates the degradation of LDLR, this inhibitor helps maintain higher levels of LDLR on the hepatocyte surface, thereby promoting the uptake of circulating LDL-C. It is a valuable tool for researching novel cholesterol-lowering therapies and cardiovascular disease prevention.

Vemtoberant, a β3 Adrenergic Receptor antagonist, is utilized in the research of disorders mediated by the β3 adrenergic receptor, including heart failure.