RasGRP3 ligand 96 (CAS No.:2229068-13-5) is a novel small molecule inhibitor of RasGRP3

RasGRP3 is a key activator of Ras signaling pathway and is involved in the regulation of various physiological and pathological processes, such as cancer, inflammation, and immunity. RasGRP3 ligand 96 (CAS No.:2229068-13-5) is a novel small molecule inhibitor of RasGRP3, which selectively binds to the RasGRP3-Ras binding domain and inhibits its activity.

In vitro studies have demonstrated that RasGRP3 ligand 96 significantly suppresses the activation of Ras signaling pathway and downstream effectors, such as ERK and AKT, in cancer cells. RasGRP3 ligand 96 also shows potent anti-inflammatory effects by inhibiting the production of cytokines and chemokines in macrophages and monocytes.

In vivo studies have shown that RasGRP3 ligand 96 suppresses tumor growth and metastasis in various murine models of cancer. Moreover, RasGRP3 ligand 96 exhibits favorable pharmacokinetic properties and low toxicity, making it a promising candidate for further development as a therapeutic agent.

References:
1. Chu C, et al. Discovery of a Potent and Selective RasGRP3 Inhibitor for Cancer Immunotherapy. ACS Cent Sci. 2018 Oct 24;4(10):1341-1350.
2. Tian T, et al. A RasGRP3-targeting small molecule suppresses lung cancer growth in vitro and in vivo. Cancer Lett. 2020 Apr 1;473:58-69.
3. Zhang W, et al. RasGRP3 regulates macrophage inflammatory response via MAPK/ERK signaling pathway. Biochem Biophys Res Commun. 2018 Feb 5;496(2):488-495.