AZ31 is a Highly Selective and Orally Active ATM Inhibitor
Ataxia telangiectasia mutated (ATM) is an ATP-dependent phosphatidylinositol 3-kinase-related kinase (PIKK) serine/threonine protein kinase. ATM is related to ATR, DNA-PKcs, mTOR, SMG1 and the non-enzymatic TRRAP within this enzyme family. Importantly, ATM is a central player in the mitotic DNA damage response (DDR), increasing the response to DNA double-strand...
CP681301 is a Potent CDK5 Inhibitor
CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. CDK5 is one of the Cyclin-dependent kinases. Importantly, CDK5 is an unconventional Cdk that regulates developmental and adult...
FPDT is an anti-glioblastoma agent and shows anti-glioblastoma activity by AKT pathway.
FPDT (2-(4-fluorophenyloamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole) is an anti-glioblastoma agent. FPDT displays cytotoxic with IC50 values of 44-68 μM for GBM cells and >100 μM for human astrocytes HA. Besides, Anti-glioblastoma activity of FPDT is linked to downregulation of the AKT pathway. FPDT (0-100 µM; 48 h) shows anti-proliferative activity with IC50 values of 53.53, 44.98, 55.20, 56.37, 67.73, >100...
Indoximod, An Immunometabolic Adjuvant, is an IDO Pathway Inhibitor
Indoleamine 2,3-dioxygenase (IDO) is an enzyme of interest in immuno-oncology. It has immunosuppressive effects that result from its role in tryptophan catabolism. IDO1 catalyzes the initial rate-limiting step in the degradation of the essential amino acid tryptophan along the kynurenine pathway. IDO inhibits a tryptophan sufficiency signal that stimulates...
AZD1390 is a Highly Selective, Orally Active and Brain-Penetrant ATM Inhibitor
Glioblastoma multiforme (GBM) is a lethal form of brain tumor arising from malignant glial cells. this disease affects 2 to 3 per 100,000 adults per year and accounts for 52% of all primary brain tumors. ATM plays a central role in the detection, signaling, and repair of DNA double-strand...
NAZ2329 is an Allosteric Inhibitor of R5 RPTP Subfamily and PTPRZ/PTPRG
The R5 subfamily of receptor protein tyrosine phosphatases (RPTPs) includes PTPRZ and PTPRG. Specifically, PTPRZ1 is a member of the receptor tyrosine phosphatase family. Besides, PTPRZ1 encodes a one-way type I membrane protein with two cytoplasmic tyrosine-protein phosphatase domains, α-carbonic anhydrase domain, and fibronectin III domain. There is a...
PINT87aa, a Potential Tumor-Suppressive Peptide, Directly Interacts with the PAF1 Complex
Circular RNAs (circRNAs) are a large class of transcripts in the mammalian genome. CircRNAs are inherently resistant to exonuclease activity (resulting in higher stability than linear RNAs) and often show tissue- or developmental stage-specific expression. It suggests that they possess important biological functions. To date, circRNAs can act as microRNA...