Telaglenastat (CB-839) is an Orally Active GLS1 Inhibitor for PDAC Cancer Research
Telaglenastat (CB-839) is a first-in-class, selective, reversible, and orally active Glutaminase-1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidneys and brains, respectively. Telaglenastat induces autophagy...
RMC-6291 is an Orally Active and Covalent KRASG12C Inhibitor for Solid Tumor Research
KRAS plays a critical role in regulating cell growth and division. KRAS mutations are common in many types of solid tumors, including lung, colon, and pancreatic cancers, and are associated with poor prognosis and limited treatment options. RMC-6291 is an orally active and covalent inhibitor of KRASG12C (ON). This...
E235 is an ATF4 Expression Regulator for Tumor Research
Activates transcription factor 4 (ATF4) is a cAMP-responsive element binding protein, belonging to the cAMP-responsive element binding protein (CREB)-2 protein family. This protein is divided into several structural domains that are crucial for the function and degradation of ATF4. Specifically, ATF4 is a stress-induced transcription factor that is frequently...
Box5 is a Potent Wnt5a Antagonist for Melanoma Research
Wnt5a (Wnt Family Member 5A) is a signaling molecule and is implicated in many different types of cancers. Importantly, Wnt5a increases intracellular Ca2+ levels and enables the activation of Ca2+-regulated proteins, such as protein kinase C (PKC) in a context-dependent manner, giving rise to the model of a non-canonical Wnt/Ca2+ signaling...
Gilteritinib (ASP2215) is a Potent and ATP-competitive FLT3/AXL Inhibitor for AML Research
Acute myeloid leukemia (AML) is a group of malignant diseases of the hematopoietic system. And, AML occurs as the result of mutations in hematopoietic stem/progenitor cells. Despite advances in treatment, AML remains a challenging disease to manage, with a high relapse rate and poor long-term outcomes. In this article,...
Galunisertib (LY2157299) is an Oral Active TGF-βRI Kinase Inhibitor
TGFβ receptors are a class of one-way serine/threonine kinase receptors. They belong to the TGFβ receptor family. TGFβ is a growth factor and cytokine involved in paracrine signaling. Importantly, it is present in many different types of tissues, including the brain, heart, kidney, liver, bone, and testis, among others....
Inavolisib is an Orally Active PI3Kα Inhibitor for Breast Cancer Research
Phosphoinositide 3-kinases (PI3Ks), also called phosphatidylinositol 3-kinases, are a family of related intracellular signal transducer enzymes. Class I PI3K enzymes consist of four distinct catalytic isoforms, PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ. The pathway, with oncogene PIK3CA and tumor suppressor gene PTEN, is implicated in the sensitivity of cancer tumors...