hdac-in-26

HDAC-IN-26, a highly selective class I HDAC inhibitor, has an EC50 value of 4.7 nM.

HDAC-IN-84 (compound 4a) is a potent HDAC inhibitor with IC50 values of 0.0045, 0.015, 0.013, 0.038, 5.8, and 26 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC11, respectively. It effectively inhibits the proliferation of leukemia cells without causing toxicity.

FLT3 VEGFR2-IN-1 (Compound 26) is a potent inhibitor of FLT3, VEGFR2, and HDAC, exhibiting IC50 values of 14.5 nM, 3.9 nM, and 30.8 nM against FLT3, VEGFR2, and HDAC1, respectively. It effectively inhibits the phosphorylation of STAT3 and ERK1 2, as well as the proliferation of leukemia cells. FLT3 VEGFR2-IN-1 demonstrates antitumor activity and is applicable in research on acute myeloid leukemia.

HDAC HSP90-IN-4 significantly inhibited HDAC and HSP90 activity, with compound 20 (HDACIC50= 194 nM; HSP90αIC50= 153 nM) and compound 26 ((HDACIC50= 360 nM; HSP90αIC50= 77 nM) having the strongest HDAC and HSP90α inhibition. effect. Both compounds induced HSP90 expression and down-regulated HSP90 client proteins, which play an important role in the regulation of cancer cell survival and invasion.

RO314724 is a HDAC inhibitor. RO314724 is also a a reversible, tightly binding, MMP inhibitor with a Ki of 26 nm. Matrix metalloproteinases (MMPs) belong to the key enzymes of the proteolytic destruction of cartilage matrix during chronic rheumatic diseases. Ro314724 displayed MMP-proteoglycanase inhibitory activity both in vitro and ex vivo and proved to be not harmful to the morphology, viability and proteoglycan biosynthesis of bovine articular cartilage explants.