Tag: KRAS

GNE-9815 is a highly selective pan-RAF inhibitor, can be used to research KRAS mutant cancers

Rapidly accelerated fibrous sarcoma (RAF) kinases are a family of three serine/threonine-specific protein kinases associated with retroviral oncogenes. They play key roles in several cellular processes, including cell cycle progression, cell proliferation, cell metabolism, cell migration, cell differentiation, and apoptosis. Activation of RAF kinases requires interaction with RAS-GTPases. RAF...

IACS-15414 is an Orally Active SHP2 Inhibitor

Src-homology-2-containing protein tyrosine phosphatase 2 (SHP2), encoded by the PTPN11 gene, is a classical nonreceptor protein tyrosine phosphatase (PTP). SHP2 is a ubiquitous protein tyrosine phosphatase with a relatively conserved structure and function. It has emerged as a key downstream regulator of several receptor tyrosine kinases (RTKs) and cytokine...

Repotrectinib is a potent ROS1 and TRK Inhibitor

Repotrectinib is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. The IC50 values are 0.83/0.05/0.1 nM for TRKA/B/C, respectively. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib inhibits mutant ALKs. It inhibits ALK G1202R with an IC50 of 1.26 nM. Besides, it inhibits ALK L1196M with an IC50 of 1.08 nM)....

LJI308 is a Pan-Ribosomal S6 Kinase (RSK) Inhibitor

The cold shock protein Y-box binding protein-1 (YB-1) is a multifunctional protein. It shows relations in cell proliferation, survival, and stress response. Through translation and transcription of key proteins and regulation of DNA repair, YB-1 performs its functions in different cancers. YB-1 displays overexpression in many tumor entities, especially...

SMAP-2 (DT-1154) is an Orally Bioavailable PP2A Activator

Protein Phosphatase 2A (PP2A) is a serine/threonine phosphatase. It regulates multiple signaling cascades implicated in cancer progression, including downstream effectors of KRAS. Inhibition of PP2A contributes to oncogenesis in multiple tumor types, highlighting the importance of this protein in maintaining normal kinase activity. Pancreatic ductal adenocarcinoma (PDA) cells have...

DT-061 is an Orally Active PP2A Activator

Protein phosphatase 2A (PP2A) comprises a family of serine/threonine phosphatases, minimally containing a well-conserved catalytic subunit. PP2A plays a prominent role in the regulation of specific signal transduction cascades. Additionally, PP2A interacts with a substantial number of other cellular and viral proteins. DT-061 is an orally bioavailable small-molecule activator...

BI-3406 is an Orally Active and Selective KRAS and SOS1 Interaction Inhibitor

KRAS functions as a molecular switch, cycling between inactive (GDP-bound) and active (GTP-bound) states to transduce extracellular signals via cell-surface receptors. KRAS signaling occurs through engagement with effector proteins that orchestrate intracellular signaling cascades regulating tumor cell survival and proliferation. Mutations in the KRAS gene occur in approximately one of seven...