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Staurosporine

Cat. No. M2066
Staurosporine Structure
Synonym:

AM-2282

Size Price Availability Quantity
2mg USD 105 In stock
5mg USD 200 In stock
10mg USD 340 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Staurosporine (antibiotic AM-2282 or STS) is a therapeutic agent that inhibits tumor cell growth by inducing cell death via intrinsic apoptotic pathways. Staurosporine is a prototypical ATP-competitive kinase inhibitor in that it binds to many kinases with high affinity, though with little selectivity. Staurosporine also inhibits a variety of other protein kinases, including PKA, PKG, phosphorylase kinase, S6 kinase, MLCK, CAM PKII, cdc2, v-Src, Lyn, c-Fgr and Syk with IC50 values 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. Staurosporine induces apoptosis of human foreskin fibroblasts AG-1518, depending on the lysosomal cathepsins D mediated cytochrome c release and caspase activation. Moreover, Staurosporine triggers a novel intrinsic apoptosis pathway, relying on the activation of caspase-9 in the absence of Apaf-1.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 466.53
Formula C28H26N4O3
CAS Number 62996-74-1
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Food Chem (2017). Figure 3. Staurosporine (Abmole Bioscience,Houston, TX, USA)
Method Measured myofibril fragmentation index
Cell Lines Muscles
Concentrations 0.144 μmol/5 g
Incubation Time 2 h, 1 d, 2 d, 3 d, 5 d and 7 day
Results During the MFI increased phase (measured at 2 h and 1 d), the MFI values of the low phosphorylation level group (protein kinase inhibited group) were significantly higher (p < 0.05) than those of the control group, while the MFI values of the high phosphorylation level group (phosphatase inhibited group) were significantly lower (p < 0.05) than those of the control group.
Rating
Source Food Chem (2017). Figure 2. Staurosporine (Abmole Bioscience,Houston, TX, USA)
Method Global phosphorylation level of myofibrillar proteins
Cell Lines Muscles
Concentrations 0.144 μmol/5 g
Incubation Time 2 h, 1 d, 2 d, 3 d, 5 d and 7 day
Results Inhibition of protein kinase by M2066 significantly reduced the phosphorylation level of myofibrillar proteins in muscle compared to control.
Rating
Source Food Chemistry (2016).Figure 4. kinase inhibitors (M2066, Abmole, Houston, TX, USA)
Method Lactic acid concentrations
Cell Lines
Concentrations 0.144 μmole per 5 g muscle pieces
Incubation Time 2h, 24h, 48h, 72h, 120h and 168h
Results No difference was observed in lactic acid content (Fig. 4) between C1 and C2 control groups. In addition, no difference in lactic acid was detected between phosphatase inhibition group and the two control groups at most time points, but the kinase inhibition group had lower lactic acid content than the other three groups (P < 0.05) throughout the entire experimental period.
Rating
Source Food Chemistry (2016).Figure 3. kinase inhibitors (M2066, Abmole, Houston, TX, USA)
Method PH Value
Cell Lines
Concentrations 0.144 μmole per 5 g muscle pieces
Incubation Time 2h, 24h, 48h, 72h, 120h and 168h
Results There was no difference in pH values (Fig. 3) between the phosphatase inhibition group and the two control groups. the pH of the kinase inhibition group declined much slower during the early postmortem stage (P < 0.05) as compared to the other three groups.
Rating
Source Food Chemistry (2016).Figure 2. kinase inhibitors (M2066, Abmole, Houston, TX, USA)
Method protein phosphrylation assay
Cell Lines
Concentrations 0.144 μmole per 5 g muscle pieces
Incubation Time 2h, 24h, 48h, 72h, 120h and 168h
Results The R630/580 values (Fig. 2) were not different between C1 and C2 control groups at any time. However, the R630/580 values of the phosphatase inhibition group were lower than those of all other groups (P < 0.05) except at 2 h. Kinase inhibition group demonstrated greater (P < 0.05) R630/580 values than those of the rest groups except at 2 and 168 h.
Rating
Source Food Chemistry (2016).Figure 1. kinase inhibitors (M2066, Abmole, Houston, TX, USA)
Method Gel electrophoresis and image analyses
Cell Lines
Concentrations 0.144 μmole per 5 g muscle pieces
Incubation Time 2h, 24h, 48h, 3d, 5d and 7d
Results "As expected, the overall phosphorylation of sarcoplasmic proteins in the minced meat with phosphatase inhibitor was significantly higher (P < 0.05) than in control and kinase inhibitor added samples."
Rating
Product Citations
References

Triggering of a novel intrinsic apoptosis pathway by the kinase inhibitor staurosporine: activation of caspase-9 in the absence of Apaf-1.
Manns J, et al. FASEB J. 2011 Sep;25(9):3250-61. PMID: 21659556.

Induction of apoptosis by staurosporine involves the inhibition of expression of the major cell cycle proteins at the G(2)/m checkpoint accompanied by alterations in Erk and Akt kinase activities.
Antonsson A, et al. Anticancer Res. 2009 Aug;29(8):2893-8. PMID: 19661292.

Staurosporine induces apoptosis of melanoma by both caspase-dependent and -independent apoptotic pathways.
Zhang XD, et al. Mol Cancer Ther. 2004 Feb;3(2):187-97. PMID: 14985459.

Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase.
Tamaoki T, et al. Biochem Biophys Res Commun. 1986 Mar 13;135(2):397-402. PMID: 3457562.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Staurosporine, AM-2282 supplier, PKC, inhibitors

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