SHR2415 is a Selective and Orally Active ERK1/2 Inhibitor

ERKs (extracellular signal-regulated kinases) are the original members of the mitogen-activated protein kinase (MAPK) family. They take part in the regulation of meiosis, mitosis, and postmitotic functions, thus, also influencing the development of cancer. ERK1 and ERK2 are important downstream points of the RAS-RAF-MEK-ERK signaling pathway. The two targets...

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...

ARD-69 is a Potent PROTAC Androgen Receptor Degrader

Androgen receptor (AR) is a ligand-dependent nuclear transcription factor and a member of the steroid hormone nuclear receptor family. In fact, AR has many biological functions and can control the expression of specific genes. AR can interact with its natural ligands 5α-Dihydrotestosterone (DHT) binds to testosterone. Importantly, AR signal...

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...

Simmiparib is An Orally Active PARP1/2 Inhibitor

Poly (ADP-ribose) polymerase (PARP), a family of proteins, is involved in various cellular processes such as DNA repair and programmed cell death. PARP is present in the cell nucleus. It consists of a DNA-binding domain, a caspase-cleaved domain, an auto-modification domain, and a catalytic domain. In particular, the protein...

G12Si-5 is a K-Ras G12S Mutant Covalent Inhibitor

KRAS (Kirsten rat sarcoma virus) is one of the most commonly altered oncogenes in human cancers. Recurrent oncogenic mutations in KRAS can reprogram glutamine metabolism to increase the production of NADPH to control ROS. Besides, mutant KRAS promotes the expression of nucleotide synthesis genes and controls glucose uptake and...

EAI001 is a Selective Mutant EGFR Allosteric Inhibitor

Epidermal growth factor receptor (EGFR) belongs to the ErbB family of receptor tyrosine kinases (RTKs). Specifically, EGFR belongs to a receptor family, which contains three additional proteins, namely ErbB-2, ErbB-3, and ErbB-4. These proteins and EGF family growth factors form a comprehensive system. Besides, EGFR participates in cell growth...