Staurosporine(CGP 41251) (Synonyms: Stsp)

Staurosporin, a small kinase inhibitor, is an alkaloid derived from the bacterium Streptomyces staurosporeus.^[1] Staurosporine can block the ATP-binding site of the enzimes and induce apoptosis by activation of caspase-3 in higher eukaryotes.^[2]

In vitro experiment it shown that treatment with 50 nM of Staurosporin, there is a single-cell migration of breast carcinoma cells on plastic, fibronectin, or laminin surfaces.^[1] Staurosporine killed Acanthamoeba trophozoites in a dose dependent way with IC50 and IC90 values of 0.265?±?0.057 and 1.27?±?0,007?μg/mL, respectively.^[2] In vitro, treatment with a low concentration (10(-7) M) of staurosporine in cultured rat astrocytes, there is a significantly increased proportion of early apoptotic cells after regeneration in a staurosporine free medium. However, treatment with a higher (10(-6) M) concentration of staurosporine, there is further obviously increased necroptosis after regeneration in a staurosporine free medium.^[3] In vitro efficacy test it indicated that 1 μM STS was able to activate the autophagy pathway in SH-SY5Y cells.^[4] In addition, treatment with 5 to 50 μM of staurosporine, conidial cell viability decreased in a concentration-dependent manner, suggesting that staurosporine has potent antifungal activity against N. crassa conidia.^[5]

In vivo efficacy study it demonstrated that mice were treated with 3 mg/kg staurosporine via oral gavage twice a week has no effects on tumor growth. But mice were treated with the combination of 3 mg/kg staurosporine and 50 mg/kg lapatinib inhibited the tumor growth obviously.^[6]

References:
[1].Meyer FAH, et al. The Presence of Yin-Yang Effects in the Migration Pattern of Staurosporine-Treated Single versus Collective Breast Carcinoma Cells. Int J Mol Sci. 2021 Nov 4;22(21):11961.
[2].Cartuche L, et al. Staurosporine from Streptomyces sanyensis activates Programmed Cell Death in Acanthamoeba via the mitochondrial pathway and presents low in vitro cytotoxicity levels in a macrophage cell line. Sci Rep. 2019 Aug 12;9(1):11651.
[3].?imenc J, et al. Staurosporine induces apoptosis and necroptosis in cultured rat astrocytes. Drug Chem Toxicol. 2012 Oct;35(4):399-405.
[4].Brunelli F, et al. PINK1 Protects against Staurosporine-Induced Apoptosis by Interacting with Beclin1 and Impairing Its Pro-Apoptotic Cleavage. Cells. 2022 Feb 15;11(4):678.
[5].Castro A, et al. Rotenone enhances the antifungal properties of staurosporine. Eukaryot Cell. 2010 Jun;9(6):906-14.
[6].Zambrano JN, et al. Staurosporine, an inhibitor of hormonally up-regulated neu-associated kinase. Oncotarget. 2018 Nov 13;9(89):35962-35973.