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Formula | C28H26N4O3 |
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Molecular Weight | 466.53 | CAS No. | 62996-74-1 | |
Solubility (25°C)* | In vitro | DMSO | 93 mg/mL (199.34 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3. | |||||||||||
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In vitro | Staurosporine, a microbial alkaloid, significantly inhibits protein kinase C from rat brain with IC50 of 2.7 nM. Staurosporine displays strong inhibitory effect against HeLa S3 cells with IC50 of 4 nM. [1] Staurosporine also inhibits a variety of other protein kinases, including PKA, PKG, phosphorylase kinase, S6 kinase, Myosin light chain kinase (MLCK), CAM PKII, cdc2, v-Src, Lyn, c-Fgr, and Syk with IC50 of 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM, and 16 nM, respectively. [2] Staurosporine (1 μM) induces >90% apoptosis in PC12 cells. Consistently, Staurosporine treatment induces a rapid and prolonged elevation of intracellular free calcium levels [Ca2+]i, accumulation of mitochondrial reactive oxygen species (ROS), and subsequent mitochondrial dysfunction. [3] The apoptosis of MCF7 cells induced by Staurosporine can be enhanced by the expression of functional caspase-3 via caspase-8 activation and Bid cleavage. [4] Staurosporine treatment at 1 μM only partially inhibits IL-3-stimulated Bcl2 phosphorylation but completely blocks PKC-mediated Bcl2 phosphorylation. [5] Staurosporine induces apoptosis of human foreskin fibroblasts AG-1518, depending on the lysosomal cathepsins D mediated cytochrome c release and caspase activation. [6] In addition to activating the classical mitochondrial apoptosis pathway, Staurosporine triggers a novel intrinsic apoptosis pathway, relying on the activation of caspase-9 in the absence of Apaf-1. [7] | |||||||||||
In vivo | In the gerbil and rat ischemia models, Staurosporine pretreatment (0.1-10 ng) before ischemia prevents neuronal damage in a dose-dependent manner, suggesting the involvement of PKC in CAl pyramidal cell death after ischemia. [8] |
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Data from [J Biomol Screen, 2013, 18(4), 388-99]
Data from [J Biomol Screen, 2013, 18(4), 388-99]
Data from [Data independently produced by PLoS One, 2012, 7(6), e39679]
Data from [Data independently produced by , , Mol Carcinog, 2018, 57(7):886-895]
Design-rules for stapled peptides with in vivo activity and their application to Mdm2/X antagonists [ Nat Commun, 2024, 15(1):489] | PubMed: 38216578 |
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Oncogenic KEAP1 mutations activate TRAF2-NFκB signaling to prevent apoptosis in lung cancer cells [ Redox Biol, 2024, 69:103031] | PubMed: 38184997 |
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics [ Mol Syst Biol, 2024, 20(1):28-55] | PubMed: 38177929 |
Lytic bacteriophages induce the secretion of antiviral and proinflammatory cytokines from human respiratory epithelial cells [ PLoS Biol, 2024, 22(4):e3002566] | PubMed: 38652717 |
Synergy of retinoic acid and BH3 mimetics in MYC(N)-driven embryonal nervous system tumours [ Br J Cancer, 2024, 10.1038/s41416-024-02740-5] | PubMed: 38942989 |
SUMOylation controls Hu antigen R posttranscriptional activity in liver cancer [ Cell Rep, 2024, 43(3):113924] | PubMed: 38507413 |
Identification and characterization of a potent and selective HUNK inhibitor for treatment of HER2+ breast cancer [ Cell Chem Biol, 2024, S2451-9456(24)00037-0] | PubMed: 38307028 |
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