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Staurosporine

Catalog No. T6680 CAS 62996-74-1

Synonyms: Antibiotic AM-2282, AM-2282, CGP 41251

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

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Staurosporine, CAS 62996-74-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 56.00
2 mg	In stock	$ 79.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 148.00
25 mg	In stock	$ 259.00
50 mg	In stock	$ 423.00
100 mg	In stock	$ 628.00
500 mg	In stock	$ 1,350.00
1 mL * 10 mM (in DMSO)	In stock	$ 111.00

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Purity: 99.87%

Purity: 99.3%

Purity: 99.24%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.
Targets&IC50	PKCε:73 nM, PKCζ:1086 nM, PKCγ:5 nM, PKCδ:20 nM, PKCη:4 nM, PKCα:2 nM
In vitro	METHODS: Human cervical cancer cells HeLa were treated with Staurosporine (1-10 nM) for 72 h, and cell viability was measured by MTT. RESULTS: Staurosporine inhibited the proliferation of Hela cells in a dose-dependent manner, with an IC50 of about 10 nM. [1] METHODS: Human pancreatic cancer cells PaTu 8988t and Panc-1 were treated with Staurosporine (1 μM) for 3-24 h, and cell death was detected by Flow Cytometry. RESULTS: For PaTu 8988t cells, incubation with Staurosporine for 3-24 h significantly increased apoptosis and significantly decreased the number of viable cells; necrosis increased after 6-16 h. For Panc-1 cells, Staurosporine treatment significantly increased apoptosis and significantly decreased the number of viable cells after 9-24 h. The RESULTS were summarized as follows. [2] METHODS: Human hepatocellular carcinoma cells HepG2 were treated with Staurosporine (20 nmol/L) for 6-24 h. The expression levels of target proteins were detected by Western Blot. RESULTS: Staurosporine significantly inhibited the phosphorylation of mTOR and increased the expression of LC3-II, an autophagy marker protein, suggesting that Staurosporine activates autophagy effectively by inhibiting mTOR. [3]
In vivo	METHODS: To assay anti-tumor activity in vivo, Staurosporine (3 mg/kg) and Lapatinib (50 mg/kg) were administered by gavage twice a week for two weeks to Nu/J-Foxn1 Nu/Nu mice harboring human mammary carcinoma tumors JIMT-1. RESULTS: The combination of Staurosporine and Lapatinib inhibited tumor growth in a statistically significant manner. [4] METHODS: To examine the effects on islet β-cell function, Staurosporine (0.4 mg/kg in 0.5% sodium carboxymethyl cellulose) was administered intraperitoneally to iPLA2β-/- C57BL6 mice once daily for two weeks. for two weeks. RESULTS: Staurosporine impairs glucose tolerance and glucose-stimulated insulin secretion in pancreatic islets. [5]
Kinase Assay	Enzyme assay and binding assay: Protein kinase C is assayed in a reaction mixture (0.25 mL) containing 5 μmol of Tris/HCl, pH 7.5, 2.5 μmol of magnesium acetate, 50 μg of histone II S, 20 μg of phosphatidylserine, 0.88 μg of diolein, 125 nmol of CaCl2, 1.25 nmol of [γ-32]ATP (5-10 × 104 cpm/nmol) and 5 μg of partially purified enzyme. The binding of [3H]PDBu to protein kinase C is determined: Reaction mixture (200 μL contained 4 μmo1 of Tris/malate, pH 6.8, 20 μmol of KCl, 30 nmol of CaC12, 20 μg of phosphatidylserine, 5 μg of partially purified protein kinase C, 0.5% (final concentration) of DMSO,10 pmol of [3H]PDBu (l-3 × 104 cpm/pmol) and 10 μL of various amounts of Staurosporine.
Cell Research	Cells are exposed to Staurosporine for ~32 hours. Cells are fixed in 4% paraformaldehyde and stained with the DNA-binding dye Hoechst 33342. Cells are visualized under epifluorescence illumination, and the percentage of apoptotic cells (cells with condensed and fragmented DNA) is determined. (Only for Reference)

Synonyms	Antibiotic AM-2282, AM-2282, CGP 41251
Molecular Weight	466.53
Formula	C28H26N4O3
CAS No.	62996-74-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 31 mg/mL (66.45 mM)

References and Literature

1. Ma X, et al. Staurosporine targets the Hippo pathway to inhibit cell growth. J Mol Cell Biol. 2018 Jun 1;10(3):267-269. 2. Malsy M, et al. Staurosporine induces apoptosis in pancreatic carcinoma cells PaTu 8988t and Panc-1 via the intrinsic signaling pathway. Eur J Med Res. 2019 Jan 28;24(1):5. 3. Ding Y, et al. Staurosporine suppresses survival of HepG2 cancer cells through Omi/HtrA2-mediated inhibition of PI3K/Akt signaling pathway. Tumour Biol. 2017 Mar;39(3):1010428317694317. 4. Zambrano JN, et al. Staurosporine, an inhibitor of hormonally up-regulated neu-associated kinase. Oncotarget. 2018 Nov 13;9(89):35962-35973. 5. Zhao Z, et al. Protection of pancreatic beta-cells by group VIA phospholipase A(2)-mediated repair of mitochondrial membrane peroxidation. Endocrinology. 2010 Jul;151(7):3038-48. 6. Yang J B, Song Y F, Liu Y, et al. UHPLC-QQQ-MS/MS assay for quantification of dianthrones as potential toxic markers of Polygonum multiflorum Thunb: Application to the standardization of TCMs with endogenous toxicity[J]. 2021 7. Xiao Q, Ye T, Wang X, et al. A network pharmacology-based study on key pharmacological pathways and targets of Qi Fu Yin acting on Alzheimer's disease[J]. Experimental Gerontology. 2021: 111336.

Citations

1. Lü Z, Li X, Li K, et al. Nitazoxanide and related thiazolides induce cell death in cancer cells by targeting the 20S proteasome with novel binding modes. Biochemical Pharmacology. 2022: 114913. 2. Yang G, Wan P, Xiang Q, et al. E3 Ubiquitin Ligase ASB17 Promotes Apoptosis by Ubiquitylating and Degrading BCLW and MCL1. Biology-Basel. 2021, 10(3): 234. 3. Yang J B, Song Y F, Liu Y, et al. UHPLC-QQQ-MS/MS assay for quantification of dianthrones as potential toxic markers of Polygonum multiflorum Thunb: Application to the standardization of TCMs with endogenous toxicity. Chinese Medicine. 021 Jul 3;16(1):51. doi: 10.1186/s13020-021-00463-w. 4. Xiao Q, Ye T, Wang X, et al. A network pharmacology-based study on key pharmacological pathways and targets of Qi Fu Yin acting on Alzheimer's disease. Experimental Gerontology. 2021 Jul 1;149:111336. doi: 10.1016/j.exger.2021.111336. Epub 2021 Mar 27. 5. Jiang X, Teng X, Shi H, et al.Discovery and optimization of olanzapine derivatives as new ferroptosis inhibitors.Bioorganic Chemistry.2023: 106393. 6. Liu H, Chen M, Ning F, et al.Extravillous trophoblast cell derived exosomes induce vascular smooth muscle cell apoptosis via a mechanism associated with miR-143-3p.Molecular Human Reproduction.2023: gaad026. 7. Tschuck J, Theilacker L, Rothenaigner I, et al.Farnesoid X receptor activation by bile acids suppresses lipid peroxidation and ferroptosis.Nature Communications.2023, 14(1): 6908. 8. Tan Q, Wu D, Lin Y, et al.Identifying eleven new ferroptosis inhibitors as neuroprotective agents from FDA-approved drugs.Bioorganic Chemistry.2024: 107261.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Microbial Natural Product Library Anti-Cancer Active Compound Library TGF-beta/Smad Compound Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Anti-Tumor Natural Product Library Bioactive Compound Library Angiogenesis related Compound Library Anti-Fungal Compound Library

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Keywords

Staurosporine 62996-74-1 Angiogenesis Apoptosis Chromatin/Epigenetic Cytoskeletal Signaling Microbiology/Virology Tyrosine Kinase/Adaptors Antibacterial Antibiotic Antifungal PKA Src PKC Antibiotic AM-2282 AM-2282 Protein kinase A Antibiotic AM2282 Antibiotic AM 2282 Bacterial Protein kinase C AM 2282 inhibit Inhibitor Fungal STS CGP 41251 CGP-41251 AM2282 CGP41251 inhibitor

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