Ruxolitinib (INCB018424) is an Orally Active JAK1 and JAK2 Inhibitor

The myeloproliferative neoplasms (MPNs) are a group of related clonal diseases probably arising from hematopoietic progenitor or stem cells. Patients with MPNs have an increased risk of thrombotic and bleeding complications and disease progression to acute myeloid leukemia. JAK2 is a member of the JAK family of cytoplasmic tyrosine...

Iberdomide (CC-220) is an Orally Active Cereblon (CRBN) E3 Ligase Modulator (CELMoD)

Cereblon (CRBN) is a key protein in autosomal recessive nonsyndromic mental retardation. Specifically, it plays an intermediary role in helping immunomodulatory drugs play their immunomodulatory and tumor-killing roles. Besides, CRBN is highly conserved from plants to mammals, and mRNA expression in humans, rats, and mice is common. CRBN interacts...

Trichostatin A (TSA) is a Specific Inhibitor of HDAC Class I/II

Histone deacetylases (HDACs) are enzymes that remove acetyl groups from histone and non-histone proteins. To date, 18 different mammalian HDACs have been identified and divided into four classes: the Class I Rpd3-like proteins (HDAC1, HDAC2, HDAC3, and HDAC8); the Class II Hda1-like proteins (HDAC4, HDAC5, HDAC6, HDAC7, HDAC9, and...

LY294002, a PI3K Inhibitor, is an Autophagy and Apoptosis Inducer

The phosphatidylinositol-3 OH kinase (PI3K)/Akt signaling pathway contributes to cancer survival, apoptosis, and regulating a variety of cellular processes. In particular, Akt serine/threonine kinase plays a critical role in controlling the balance between cell survival and apoptosis. Dysregulation of this pathway is frequently observed in a variety of tumors,...

Staurosporine is an ATP-competitive Inhibitor of Protein Kinases

Protein kinases are enzymes that catalyze protein phosphorylation. Obviously, Protein kinases include many types of kinases, such as  PKC,PKA, c-Fgr and phosphorylase kinase. Thereinto, PKC, PKA and phosphorylase kinase belong to serine or threonine kinases and c-Fgr belongs to Tyr kinases. Interestingly, diacylglycerol (DG) can activate PKC and the...