Tag: SHP2

BPDA2 is a Highly Selective and Competitive SHP2 Inhibitor

SH2-containing protein tyrosine phosphatase 2 (SHP2) is a carcinogenic phosphatase. Specifically, SHP2 participates in the downstream signal transmission of various RTK. So it is the shared signal node for analysis. The phosphatase activity of SHP2 is necessary for important cancer-related signaling pathways (such as RAS and PI3K). Besides, the...

GS-493 is a Selective Protein Tyrosine Phosphatase SHP2 (PTPN11) Inhibitor

The protein tyrosine phosphatase SHP2 (also called SH-PTP2, Syp, PTP1D, and PT-P2C) is a ubiquitously expressed 68 kDa non-receptor PTP. In the inactive state, the SH2 domains of SHP2 auto-inhibit the catalytic PTP domain by binding intramolecularly to the defined acidic residues. Upon activation, several receptor tyrosine kinases, including MET,...

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...

PHPS1 is a Selective Shp2 Inhibitor

SHP2 is a non-receptor protein tyrosine phosphatase (PTP) encoded by the human PTPN11 gene. Particularly, SHP2 contains a PTP catalytic domain and two SH2 domains. SHP2 is a ubiquitous PTP with a relatively conserved structure and function. Specifically, SHP2 is relevant to cell proliferation and differentiation induced by various...

SHP394 is an Orally Active and Selective Inhibitor of SHP2

SH2 containing protein tyrosine phosphatase-2 (SHP2) is an oncogenic phosphatase. SHP2 facilitates growth and survival signaling downstream of numerous receptor inputs. In addition, higher levels of SHP2 phosphorylation associate with decreased survival of breast cancer patients. Especially, SHP394 is an orally active and selective inhibitor of SHP2. Pharmacological inhibition...

IACS-13909 is a Selective and Orally Active SHP2 Inhibitor

Src homology 2 domain-containing phosphatase (SHP2) is a phosphatase that mediates signaling downstream of multiple receptor tyrosine kinases. SHP2 suppresses signaling through the MAPK pathway. Furthermore, SHP2 inhibition has demonstrated tumor growth inhibition in receptor tyrosine kinases-activated cancers. In this study, researchers report the discovery of IACS-13909. IACS-13909 is...

TNO155 is an Orally Active WT SHP2 Inhibitor with Antineoplastic Activity

SHP2 is a non-receptor ubiquitous protein tyrosine phosphatase and has a relatively conserved structure and function. The SHP2 includes the PTP domain, two SH2 domains, and a C-terminal tail containing two phosphorylation sites. Binding of the N-SH2 domain with the PTP domain is able to inhibit SHP2 activity. N-SH2...