Staurosporine
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Staurosporine（星孢菌素）是一种由链霉菌Streptomyces staurospores产生的生物碱，最初是作为抗真菌剂使用的。Staurosporine是一种广谱性的蛋白激酶抑制剂，可以抑制蛋白激酶C（PKC）、cAMP依赖性蛋白激酶（PKA）、磷酸激酶、核糖体蛋白S6激酶、表皮生长因子受体（EGF-R）激酶和Ca2+/钙调蛋白依赖性蛋白激酶II（钙/钙调PKII）。Staurosporine对PKC的抑制作用是最强的（IC50 = 2.7 nM）。Staurosporine对一些哺乳动物的肿瘤细胞系表现出很强的细胞毒性，诱导细胞凋亡，抑制裂殖酵母在细胞分裂后的伸长。
参考文献：
Takashi Toda, Mizuki Shimanuki, and Mitsuhiro Yanagida. Fission yeast genes that confer resistance to staurosporine encode an AP-1-like transcription factor and a protein kinase related to the mammalian ERK1/MAP2 and budding yeast FUS3 and KSS1 kinases. Genes Dev. 1991 5: 60-73
Michelle M. Hill, Mirjana Andelkovic, Derek P. Brazil, Stefano Ferrari, Doriano Fabbro, and Brian A. Hemmings. Insulin-stimulated protein kinase B phosphorylation on Ser-473 is independent of its activity and occurs through a Staurosporine-insensitive kinase. J. Biol. Chem 2001, 276: 25643-25646.
Flavio Meggio, Arianna Donella Deana, Maria Ruzzene, Anna M. Brunati, Luca Cesaro, Barbara Guerra, Thomas Meyer, Helmut Mett, Doriano Fabbro, Pascal Furet, Grazyna Dobrowolska, and Lorenzo A. Pinna. Different susceptibility of protein kinases to staurosporine inhibition kinetic studies and molecular bases for the resistance of protein kinase CK2. Eur. J. Biochem. 234, 317-322 (1995)
- 1. Arwen Conod, Marianna Silvano, et al. "On the origin of metastases: Induction of pro-metastatic states after impending cell death via ER stress, reprogramming, and a cytokine storm." Cell Rep. 2022 Mar 8;38(10):110490. PMID: 35263600
- 2. Ramon Edwin Caballero, Simon Xin Min Dong, et al. "Role of RIPK1 in SMAC mimetics-induced apoptosis in primary human HIV-infected macrophages." Sci Rep. 2021 Nov 25;11(1):22901. PMID: 34824340
- 3. Zintis Inde, Jason Rodencal, et al. "Quantification of drug-induced fractional killing using high-throughput microscopy." STAR Protoc. 2021 Jan 22;2(1):100300. PMID: 33532743
- 4. Chu xue, Si-Xue Liu, et al. "Corydalis Saxicola Bunting Total Alkaloids Inhibits Paclitaxel-Induced Peripheral Neuropathy By Regulating PKCε-TRPV1 and p38 MAPK-TRPV1 Signaling Pathways." Research Square. doi.org/10.21203/rs.3.rs-332970/v1.
- 5. Zintis Inde, Giovanni C. Forcina, et al. "Kinetic Heterogeneity of Cancer Cell Fractional Killing." Cell Rep. 2020 Jul 7;32(1):107845. PMID: 32640215
- 6. Zintis Inde, Giovanni C. Forcina, et al. "Large-Scale Analysis of Cell Death Phenotypic Heterogeneity." bioRxiv 2020.02.28.970079.
- 7. Waer CN, Kaur P, et al. "Rosmarinic Acid/ Blue Light Combination Treatment Inhibits Head and Neck Squamous Cell Carcinoma In Vitro." Anticancer Res. 2020;40(2):751–758. PMID: 32014917
- 8. Mikhail Chesnokov, Imran Khan, et al. "The MEK1/2 pathway as a therapeutic target in high-grade serous ovarian carcinoma." bioRxiv. 2019 September 16.
- 9. Clark R, Usselmann L, et al. "A flexible high content imaging assay for profiling macrophage efferocytosis." J Immunol Methods. 2019 Jul 29:112636. PMID: 31369739
- 10. Chung HK, Zou X, et al. "A compact synthetic pathway rewires cancer signaling to therapeutic effector release. Science." 2019 May 3;364(6439). PMID: 31048459
- 11. Ashok Kumar, Ramon Edwin Caballero, et al. "Inhibitor of apoptosis, IAP, genes play a critical role in the survival of HIV-infected macrophages." BioRxiv. 2019 February 06.
- 12. Wang Y, Li Y, et al. "The cerebral cavernous malformation disease causing gene KRIT1 participates in intestinal epithelial barrier maintenance and regulation." FASEB J. 2018 Sep 25:fj201800343R. PMID: 30252535
- 13. Nissen SK, Pedersen JG, et al. "Multiple Homozygous Variants in the STING-Encoding TMEM173 Gene in HIV Long-Term Nonprogressors." J Immunol. 2018 May 15;200(10):3372-3382. PMID: 29632140
- 14. Jarrett Smith,Geraldine Seydoux, et al. "Liquid-like P granules require ATP hydrolysis to avoid solidification." bioRxiv,Jan. 10, 2018.
- 15. Melanie Villanueva, B.Sc. "Glyoxalase 1 Attenuates the Effects of Chronic Hyperglycemia on Explant-Derived Cardiac Stem Cells." University of Ottawa.Melanie Villanueva, B.Sc.
- 16. Bozza, William P., et al. "The Use of a Stably Expressed FRET Biosensor for Determining the Potency of Cancer Drugs." PloS one 9.9 (2014): e107010. PMID: 25188024
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 466.53 |
| Cas No. | 62996-74-1 |
| Formula | C28H26N4O3 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥11.66 mg/mL in DMSO |
| Chemical Name | (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 |
| SDF | Download SDF |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验： | |
|
细胞系 |
A31、CHO-KDR、Mo-7e和A431细胞系 |
|
溶解方法 |
在DMSO中的溶解度 |
|
反应条件 |
24 h；IC50=0.08 mM（A31细胞系）、IC50=0.30 mM（Mo-7e细胞系）、IC50=1.0 mM（CHO-KDR细胞系）。 |
|
应用 |
在A31、Mo-7e和CHO-KDR细胞系中，staurosporine分别抑制血小板衍生生长因子（PDGF）、干细胞因子c-Kit和VEGF（KDR）诱导的受体自磷酸化，IC50值分别为0.08 mM、0.30 mM和1.0 mM。而在A431细胞系中，staurosporine不影响胰岛素、IGF-I或表皮生长因子（EGF）诱导的受体自磷酸化。 |
| 动物实验： | |
|
动物模型 |
无胸腺裸鼠 |
|
剂量 |
75 mg/kg/day；口服给药 |
|
应用 |
Staurosporine（75 mg/kg/day p.o.）完全抑制VEGF，而非bFGF诱导的血管生成反应。因此，staurosporine除了直接抑制肿瘤细胞增殖（通过其对PKCs的效应），还可以通过抑制肿瘤血管生成（通过其对VEGF-R酪氨酸激酶的效应），从而抑制肿瘤生长。该抗血管生成效应可能有助于抗肿瘤转移及广泛的抗肿瘤活性，正如staurosporine及其与细胞毒性剂的协同作用。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Andrejauskas-Buchdunger E, Regenass U. Differential inhibition of the epidermal growth factor-, platelet-derived growth factor-, and protein kinase C-mediated signal transduction pathways by the staurosporine derivative CGP 41251[J]. Cancer research, 1992, 52(19): 5353-5358. [2] Fabbro D, Buchdunger E, Wood J, et al. Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent[J]. Pharmacology & therapeutics, 1999, 82(2): 293-301. |
|
| 描述 | Staurosporine是一种有效的PKC抑制剂，在非细胞试验中作用于PKCα、PKCγ 和PKCη，IC50分别为2 nM、5 nM 和 4 nM。 | |||||
| 靶点 | PKCα | PKCγ | PKCη | PKCδ | PKCε | PKCζ |
| IC50 | 2 nM | 5 nM | 4 nM | 20 nM | 73 nM | 1086 nM |
质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
相关生物数据
相关生物数据
相关生物数据
相关生物数据
相关生物数据
