Category: Cancer

CMLD012073, an Amidino-Rocaglates, is a Potent eIF4A Inhibitor

The eukaryotic translation initiation factors 4A (eIF4A) is crucial for the assembly of the translationally active ribosome. Especially, the eIF4A is an RNA helicase that forms part of the machinery of translation initiation. Small molecules targeting the translation machinery show considerable promise in the treatment of a variety of...

MSA-2 is an Orally Available STING Agonist with Anti-tumor Activity

Stimulator of interferons genes (STING) is an adaptor protein. It plays a critical role in the secretion of type I interferons and pro-inflammatory cytokines in response to cytosolic nucleic acid. STING is also an endoplasmic reticulum-associated homodimeric protein. It is the receptor for cGAMP. The cGAMP is a second...

SM1-71 is a Multi-Targeted Kinase Inhibitor with Anti-Cancer Activity

In this article, we will introduce a potent TAK1 inhibitor, with a Ki of 160 nM. SM1-71 inhibits MEK1 activities with an IC50 of 142 nM. It also exhibits only weak activity against ERK2 with an IC50 of 1090 nM. Additionally, SM1-71 has an acrylamide warhead in the ortho-position. At the same time, it...

YKL-5-124 is a Selective, Irreversible and Covalent CDK7 Inhibitor

Cyclin-dependent kinase 7 (CDK7) is a member of the cyclin-dependent protein kinase (CDK) family. Specifically, CDK7 is an important component of TFIIH, which is involved in transcription initiation and DNA repair. Besides, CDK7 protein is a direct link between transcriptional regulation and cell cycle. In the cytoplasm, CDK7 contains...

JH295 is an Irreversible and Selective NIMA-Related Kinase 2 (Nek2) Inhibitor

NIMA-related kinase 2 (Nek2) is a homodimeric serine/threonine kinase. It localizes to centrosomes, the microtubule organizing centers of the cell. At the onset of mitosis, Nek2 phosphorylates the inter-centrosome linker proteins, C-Nap1, and rootletin. Nek2 plays a role in bipolar spindle assembly driven by the microtubule motor protein, Eg5....

ATH686 is a Selective and ATP-Competitive FLT3 Inhibitor

FLT3 is a kind of cytokine receptor, belonging to class III tyrosine kinase. Specifically, FLT3 signaling is important for the normal development of hematopoietic stem cells and progenitor cells. Specifically, the FLT3 gene is one of the most common mutations in acute myeloid leukemia (AML). There are high levels...

MS117 is a First-in-Class and Irreversible PRMT6 Covalent Inhibitor

PRMT6 is a protein arginine methyltransferase responsible for histone H3 arginine 2 (H3R2) methylation. PRMT6 negatively regulates DNA methylation and that PRMT6 upregulation contributes to global DNA hypomethylation in cancer. Mechanistically, PRMT6 overexpression impairs the chromatin association of UHRF1, resulting in passive DNA demethylation. Especially, PRMT6 plays an important...