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staurosporine (Antibiotic AM-2282,Stsp) 星孢菌素
貨號(hào) | ICA1041 | 售價(jià)(元) | 2998 |
規(guī)格 | 5mg | CAS號(hào) | 62996-74-1 |
- 產(chǎn)品簡介
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產(chǎn)品簡介:
Staurosporin 是一種小激酶抑制劑,是一種從細(xì)菌 Streptomyces staurosporeus 中提取的生物堿。[1] Staurosporine 可以阻斷酶的 ATP 結(jié)合位點(diǎn),并通過激活 caspase-3 誘導(dǎo)細(xì)胞凋亡在高等真核生物中。[2]
體外實(shí)驗(yàn)表明,50 nM Staurosporin 處理后,乳腺癌細(xì)胞在塑料、纖連蛋白或?qū)诱尺B蛋白表面出現(xiàn)單細(xì)胞遷移。[1] Staurosporine 殺死棘阿米巴滋養(yǎng)體呈劑量依賴性,IC50 和 IC90 值分別為 0.265 ± 0.057 和 1.27 ± 0,007 μg/mL。[2] 在體外,用低濃度 (10(-7) M) 處理在培養(yǎng)的大鼠星形膠質(zhì)細(xì)胞中,星形膠質(zhì)細(xì)胞在不含星形膠質(zhì)細(xì)胞的培養(yǎng)基中再生后,早期凋亡細(xì)胞的比例顯著增加。然而,用更高(10(-6) M)濃度的星形孢菌素處理,在無星形孢菌素培養(yǎng)基中再生后壞死性凋亡進(jìn)一步明顯增加。[3]體外藥效試驗(yàn)表明,1 μM STS 能夠激活 SH-SY5Y 細(xì)胞的自噬途徑。[4] 此外,用 5 至 50 μM 星形孢菌素處理后,分生孢子細(xì)胞活力呈濃度依賴性下降,表明星形孢菌素對 N. crassa 分生孢子具有有效的抗真菌活性。[5]
體內(nèi)功效研究表明,每周兩次通過口服強(qiáng)飼法以 3 mg/kg 星形孢菌素處理小鼠對腫瘤生長沒有影響。但小鼠用 3 mg/kg 星形孢菌素和 50 mg/kg 拉帕替尼聯(lián)合治療可明顯抑制腫瘤生長。[6]
產(chǎn)品性質(zhì):
Cas No.:62996-74-1
別名:星形孢菌素; Antibiotic AM-2282; STS; AM-2282
化學(xué)名: (5S,6R,7R,9R)-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-14(5H)-one
Canonical SMILES: O=C(NC1)C2=C1C3=C(C4=C2C5=C(C=CC=C5)N4[C@H]6C[C@@H](NC)[C@@H](OC)[C@]7(C)O6)N7C8=CC=CC=C83
分子式:C28H26N4O3
分子量:466.53
溶解度:≥ 11.6mg/mL in DMSO
儲(chǔ)存條:Store at -20°C
注意事項(xiàng):
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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.