JS25, a Selective and Covalent BTK Inhibitor, Acts by Segregating Tyr551
BTK, Bruton’s tyrosine kinase, belongs to the cytoplasmatic kinases TEC subfamily. BTK involves in immune regulation, and is activated by Src kinases. Then BTK leads to phospholipase-Cγ (PLCγ) phosphorylation, Ca2+ mobilization, and NF-κB/MAP activation. Meanwhile, BTK increases proinflammatory cytokines IL-6 and IL-10 production and controls integrin-mediated B-cells adhesion. Moreover,...
Purinostat mesylate is a Selective HDAC Inhibitor With anti-Leukemia Effects
Purinostat mesylate is a selective inhibitor of HDAC. This compound inhibits class I and class IIb HDACs with IC50s from 0.81 to 11.5 nM. Purinostat mesylate (1-10 μM) inhibits HDAC1, 2, 3, and 8. And the IC50s are 0.81, 1.4, 1.7, and 3.8 nM, respectively. It also inhibits HDAC6 and 10,...
TK4g is a JAK Inhibitor for Leukemia Cancer Research
Janus kinase (JAK) is an intracellular non-receptor tyrosine kinase. There are four members of the JAK family: JAK1, JAK2, JAK3, and Tyrosine kinase 2 (TYK2). JAK can link cytokine signals from membrane receptors to activators of transcription (STAT), transducing cytokine-mediated signals via the JAK-STAT signaling pathway. When the receptor...
DD1 is a Proteasome Inhibitor Used for Acute Myeloid Leukemia (AML) Research
Acute myeloid leukemia (AML) is clinically and genetically heterogeneous hematopoietic cancer. Leukemia cells are unable to undergo growth arrest and terminal differentiation. The conventional chemotherapeutic approach for AML contains a combination of anthracycline with cytarabine. However, due to either refractory to front-line therapy or subsequent relapse, AML remains a...
Daunorubicin is a Topoisomerase II Inhibitor with potent Antineoplastic Activities
Topoisomerases are enzymes that regulate the overwinding or underwinding of DNA. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. Topoisomerases are isomerase enzymes that act on the topology of DNA. Type I topoisomerase cuts one strand of a DNA double helix, relaxation...
MRT199665 is a ATP-Competitive MARK/SIK/AMPK Inhibitor
In acute myeloid leukemia (AML), chemotherapy resistance remains prevalent and poorly understood. AML are cancers of the blood. They originate in the hematopoietic progenitor cells as a result of the accumulation of genetic mutations that lead to cell transformation. Prevalence of mutations of genes encoding regulators of gene expression...
MPT0B392 Induces Apoptosis via Inhibiting Tubulin Polymerization and Inducing c-JNK Activation
Acute leukemia is a neoplastic disease characterized by a rapid accumulation of primitive hematopoietic cells. MPT0B392 acts as a potential anticancer drug for the treatment of acute leukemia. MPT0B392 is a strong microtubule binding and depolymerizing agent but not a p-gp substrate. To determine the antitumor activity of MPT0B392,...