Taspine

Product description: Taspine is an alkaloid with multifunctional pharmacological properties, including apoptosis-inducing, anti-angiogenic, anticancer, cytotoxic, anti-inflammatory and wound-healing activities, thereby modulating multiple targets. Taspine is a potent acetylcholinesterase (AChE) inhibitor and wound healing promoter (cicatrizant), by regulating the expression of keratinocyte growth factor (KGF; FGF-7) in early phases. Taspine has anticancer properties targeting DNA topoisomerase IB and was shown to be a dual topoisomerase inhibitor. Taspine is an apoptosis-inducing compound. It induces conformational activation of the pro-apoptotic proteins Bak and Bax, mitochondrial cytochrome c release and mitochondrial membrane permeabilization. It induced tumor apoptosis in vitro and in vivo. Taspine can inhibit tumor angiogenesis acting as a multi-target VEGFR-2 inhibitor. Taspine was shown to downregulate VEGF expression and inhibit the proliferation of vascular endothelial cells through PI3 kinase and MAPK signaling pathways. The anti-angiogenic activity of taspine may depend on its EGF secretion properties and therefore the modulation of the EGFR signaling pathways, mediating MAPK (Erk1/2) but Akt signals. Taspine is a human P2X4 receptor inhibitor, mediating its effect through PI3-kinase inhibition. Activation of P2X4 is associated with inflammation involving peripheral and central inflammatory cell types. It also has been shown to act as a potent TLR2 antagonist, contributing to its anti-inflammatory properties.

Alternate Names/Synonyms: Thaspine; NSC 76022; NSC 618155; NSC 688259

CAS: 602-07-3

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