Category: Hematological Malignancies

SZUH280 is a Potent And Selective PROTAC HDAC8 Degrader

Histone deacetylase 8 (HDAC8) is a class I histone deacetylase. Unlike other class I HDACs, it localizes both in the nucleus and in the cytoplasm. HDAC8 can also target non-histone proteins, such as the structural maintenance of chromosome 3 (SMC3) cohesin protein, retinoic acid induced 1 (RAI1) and p53....

Ganetespib (STA-9090) is a HSP90 Inhibitor

Hsp90 is a molecular chaperone that regulates the posttranslational folding, stability, and function of its protein substrates (client proteins), many of which play critical roles in cell growth, differentiation, and survival. The Hsp90 machinery serves as a biochemical buffer for a number of oncogenic signaling proteins causally implicated in...

OT-82 is an Orally Active NAMPT Inhibitor with Antineoplastic Activity

Treatment of hematopoietic (HP) malignancies such as leukemia, lymphoma, and myeloma need improvement due to the drug high toxicity. Some effective anticancer agents are tissue-selective but not cancer-specific targets. These agents cannot distinguish normal and transformed cells. Besides they are usually against lineage-specific metabolic deficiency or lineage-specific surface antigen,...

CM-272, a First-in-class, Reversible and Dual G9a/DNMTs Inhibitor

Therapy of hematological malignancies is undergoing a paradigm shift. It is away from the traditional chemotherapy towards the targeting of proteins driving the cancer phenotype. The novel therapeutic approach relies on the use of epigenetic drugs. It aims to reverse critical epigenetic events underlying human cancer pathogenesis, particularly abnormalities...

CC-223 is an Orally Bioavailable mTOR Kinase Inhibitor

mTOR is a serine/threonine kinase that regulates cell growth, metabolism, proliferation, and survival. mTORC1 is a master regulator of cell growth and metabolism. mTORC1 positively regulates cell growth and proliferation. mTORC2 regulates cytoskeletal organization. CC-223 is a potent mTOR kinase inhibitor with an IC50 of 0.016 μM. CC-223 is...