Silmitasertib is a CK2 Inhibitor for Hematological Tumor Research
Casein kinase 2 is a serine/threonine selective protein kinase. Firstly, CK2 typically appears as a tetramer of two α subunits; α is 42 kDa, α' is 38 kDa, and two…
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…
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…
SG3199, an ADC Cytotoxin, is a Cytotoxic DNA Minor Groove Interstrand Crosslinking PDB Dimer
The pyrrolobenzodiazepines (PBD) are a class of compound that may have antibiotic or anti-tumor properties. They exert their biological activity by binding in the minor groove of DNA. PBD dimers…
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…
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…
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.…
TAS4464, a Highly Potent and Selective Inhibitor of NEDD8 Activating Enzyme, Shows Antitumor Activity
TAS4464, a highly potent and selective inhibitor of NEDD8 activating enzyme, shows antitumor activity. NEDD8 activating enzyme (NAE) is an essential regulator of the NEDD8 conjugation pathway. The ubiquitin-like modifier…
Alisertib is an Oral Active and Selective Aurora A Kinase Inhibitor
As we all know, Alisertib (MLN8237) is an orally available selective aurora A kinase inhibitor. Aurora kinases are essential mediators in cell mitosis. Amplification of these kinases can lead to…