Talacotuzumab is an IgG1 CD123-Neutralizing Monoclonal Antibody
Interleukin-3 receptor (CD123) is a soluble cytokine that is important for the immune system. CD123 is the receptor of interleukin 3 α Chain is a cytokine receptor. Meanwhile, CD123 is overexpressed in a variety of hematological malignancies. Compared with non-tumor hematopoietic stem cells, CD123 expression was high in leukemia...
Rohinitib is a Specific eIF4A Inhibitor Used for Acute Lymphoblastic Leukemia Research
eIF4A is an enzymatic core of the eIF4F complex and an indispensable effector of the mTORC1 pathway. In the first place, eIF4A is a popular target for cancer treatments. Due to the inhibitory effect to translation initiation, eIF4A represses the oncogenic activation of HSF1. Moreover, HSF1 is a factor...
Olutasidenib, a Brain-Penetrant Mutant IDH1 Selective Inhibitor For AML Research
On December 1, 2022, FDA approved Rezlidhea (Olutasidenib) to treat adults with relapsed or refractory acute myeloid leukemia (AML) with a susceptible (IDH1) mutation. Olutasidenib (FT2102) is a highly potent, orally active, brain-penetrant, and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1). As a result, The IC50 values are...
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...
Pulrodemstat is a Potent, Selective, Reversible and Orally Active Inhibitor of LSD1
Lysine-specific histone demethylase 1A (LSD1) also known as lysine (K)-specific demethylase 1A (KDM1A) is a protein in humans that is encoded by the KDM1A gene. LSD1 is a member of a broad family of monoamine oxidases that requires FAD as a cofactor to catalyze demethylase activity. In addition, LSD1...