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Staurosporine(CGP 41251)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Staurosporine(CGP 41251)图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议

产品介绍
Staurosporine(CGP 41251) 是一种有效的 ATP 竞争性和非选择性蛋白激酶抑制剂,对 PKC、PKA、c-Fgr 和磷酸化酶激酶的 IC50 分别为 6 nM、15 nM、2 nM 和 3 nM。

Cell lines

THP-1 cells

Preparation Method

THP-1 cells were plated at 4 × 106cells per ml in 6- or 24-well plates for performing the caspase 3 fluorometric assay or in 8-well chamber slides for the TUNEL assay.Live or dead microsporidia spores were added to wells at a parasite to host cell ratio of 3:1. Apoptosis was experimentally induced by treatment with 1 uM of staurosporine after 4 h.

Reaction Conditions

1 uM; 4h

Applications

Macrophages incubated with live E. cuniculi and induced by staurosporine exhibited significantly fewer TUNEL-positive cells compared to macrophages incubated without microsporidia and induced with staurosporine.

Animal models

female immunocompromised mice, Nu/J-Foxn1 nu/nu

Preparation Method

When tumors reached a volume of - 65 mm3, mice were randomized into one of four treatment groups: placebo, staurosporine, lapatinib, or combined staurosporine and lapatinib. For the staurosporine single and combination treatment groups, mice received 3 mg/kg staurosporine via oral gavage twice a week. For the lapatinib single and combination treatment groups, mice received 50 mg/kg lapatinib via oral gavage twice a week. Tumor measurements were taken twice weekly on the days of treatment./p>

Dosage form

3 mg/kg; p.o.

Applications

Staurosporine by itself showed no effects on tumor growth, likely due to the fact that we used a low dose of staurosporine (3 mg/kg). However, the combination of 3 mg/kg staurosporine and 50 mg/kg lapatinib impaired tumor growth in a statistically significant manner.

文献引用
产品描述

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].Simenc 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.