Staurosporine(CGP 41251)
(Synonyms: 星形孢菌素; Antibiotic AM-2282; STS; AM-2282) 目录号 : GC15299
Staurosporin 是一种小激酶抑制剂，是一种从细菌 Streptomyces staurosporeus 中提取的生物碱。
Cas No.:62996-74-1
Sample solution is provided at 25 µL, 10mM.
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.
Staurosporin 是一种小激酶抑制剂,是一种从细菌 Streptomyces staurosporeus 中提取的生物碱。[1] Staurosporine 可以阻断酶的 ATP 结合位点,并通过激活 caspase-3 诱导细胞凋亡在高等真核生物中。[2]
体外实验表明,50 nM Staurosporin 处理后,乳腺癌细胞在塑料、纤连蛋白或层粘连蛋白表面出现单细胞迁移。[1] Staurosporine 杀死棘阿米巴滋养体呈剂量依赖性,IC50 和 IC90 值分别为 0.265 ± 0.057 和 1.27 ± 0,007 μg/mL。[2] 在体外,用低浓度 (10(-7) M) 处理在培养的大鼠星形胶质细胞中,星形胶质细胞在不含星形胶质细胞的培养基中再生后,早期凋亡细胞的比例显着增加。然而,用更高（10(-6) M）浓度的星形孢菌素处理,在无星形孢菌素培养基中再生后坏死性凋亡进一步明显增加。[3]体外药效试验表明,1 μM STS 能够激活 SH-SY5Y 细胞的自噬途径。[4] 此外,用 5 至 50 μM 星形孢菌素处理后,分生孢子细胞活力呈浓度依赖性下降,表明星形孢菌素对 N. crassa 分生孢子具有有效的抗真菌活性。[5]
体内功效研究表明,每周两次通过口服强饲法以 3 mg/kg 星形孢菌素处理小鼠对肿瘤生长没有影响。但小鼠用 3 mg/kg 星形孢菌素和 50 mg/kg 拉帕替尼联合治疗可明显抑制肿瘤生长。[6]
| Cell experiment [1]: | |
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Cell lines |
THP-1 cells |
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Preparation Method |
THP-1 cells were plated at 4 × 106 cells 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. |
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Reaction Conditions |
1 uM; 4h |
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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 experiment [2]: | |
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Animal models |
female immunocompromised mice, Nu/J-Foxn1 nu/nu |
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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> |
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Dosage form |
3 mg/kg; p.o. |
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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. |
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References: [1].Sokolova YY, et al. Encephalitozoon cuniculi and Vittaforma corneae (Phylum Microsporidia) inhibit staurosporine-induced apoptosis in human THP-1 macrophages in vitro. Parasitology. 2019 Apr;146(5):569-579. [2].Zambrano JN, et al. Staurosporine, an inhibitor of hormonally up-regulated neu-associated kinase. Oncotarget. 2018 Nov 13;9(89):35962-35973. |
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| Cas No. | 62996-74-1 | SDF | |
| 别名 | 星形孢菌素; Antibiotic AM-2282; STS; AM-2282 | ||
| 化学名 | (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 | 储存条件 | Store at -20°C |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1435 mL | 10.7174 mL | 21.4348 mL |
| 5 mM | 0.4287 mL | 2.1435 mL | 4.287 mL |
| 10 mM | 0.2143 mL | 1.0717 mL | 2.1435 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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Quality Control & SDS
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Related Biological Data
Morphology of HNSCC cells after ferroptosis-inducer treatment.(G)HNSCC cells were treated with DMSO, 5µ MErastin, 5µ MRSL3, or 200nM STS for 24h, with or without 5µ Mliproxstatin-1 treated for 2 h in advance.
HNSCC cells were treated with DMSO, 5µ MErastin, 5µ MRSL3, or 200nM STS(GlpBio) for 24h, with or without 5µ Mliproxstatin-1 treated for 2 h in advance.
Int J Mol Sci 23.16 (2022): 9014. PMID: 36012290 IF: 6.2082 -
Related Biological Data
Erastin and RSL3 induce ferroptosis but not apoptosis and N2A cells. (E)The viability of N2A cells was measured after treating with DMSO, 2 µM Erastin, 1 µM RSL3, or 200 nM apoptosis inducer staurosporine (STS), or combination with 20 µM apoptosis inhibitor Z-VAD-FMK (Z-VAD) for 24 h.
The viability of N2A cells was measured after treating with DMSO, 2 µM Erastin, 1 µM RSL3, or 200 nM apoptosis inducer staurosporine (STS)(GlpBio), or combination with 20 µM apoptosis inhibitor Z-VAD-FMK (Z-VAD) for 24 h.
Int J Mol Sci 22.16 (2021): 8898. PMID: 34445601 IF: 5.923