Staurosporine-Antibiotic-AM-2282-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEStaurosporineCat. No.: HY-15141CAS No.: 62996-74-1Synonyms: Antibiotic AM-2282; STS; AM-2282分式: CHNO分量: 466.53作靶點(diǎn): PKC; PKA作通路: Epigenetics; TGF-beta/Smad; Protein Tyrosine Kinase/RTK;Stem Cell/Wnt儲(chǔ)存式: Powder -20C 3 years4C 2 ye

2、arsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 31 mg/mL (66.45 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.46 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.46 mM); Clear solutionBIOLOG

3、ICAL ACTIVITY物活性 Staurosporine種有效，選擇性蛋激酶抑制劑，抑制 PKC，PKA，c-Fgr，和 Phosphorylase kinase 的IC50 分別為 6 nM，15 nM，2 nM，3 nM。IC50 & Target PKC PKA c-Fgr Phosphorylase kinase6 nM (IC50) 15 nM (IC50) 2 nM (IC50) 3 nM (IC50)S6 kinase (70 kDa) v-Src cdc2 TPK-IIB/Syk5 nM (IC50) 6 nM (IC50) 9 nM (IC50) 16 nM (IC50)

4、Ca2+/CaM PK-I1 MLCK IR EGF-R20 nM (IC50) 21 nM (IC50) 61 nM (IC50) 100 nM (IC50)ERK-1 CSK IGF-IR CK21500 nM (IC50) 2000 nM (IC50) 6150 nM (IC50) 19500 nM (IC50)CK1163500 nM (IC50)體外研究 Staurosporine, widely used as a protein kinase C (PKC) inhibitor with a broad spectrum of activity, is analkaloid is

5、olated from the culture broth of Streptomyces staurospores. MC3T3E-1 osteoblasts, expose toStaurosporine (100 nM) for 12 h, release an amount of LDH (12.43.1%) that is similar to that release by thecontrol cells(10.02.4%), indicating the relative absence of lytic death, which occurs in necrosis. In

6、addition,treatment with Staurosporine (100 nM) results in morphological changes, characteristic of apoptosis: abrightblue fluorescent condensed nuclei seen through a fluorescence microscope after Hoechst 33258-staining, and a reduction of cell volume 2.體內(nèi)研究 The inhibitory effect of Staurosporine is

7、statistically significant at around Wk 10 of tumor promotion. Althoughstatistically significant inhibition is not obtained with 10 ng of Staurosporine in later weeks of the experiment,a decreasing tendency in the percentages of tumor bearing mice and in average numbers of tumors permouse is apparent

8、. Thus, Staurosporine slightly inhibits tumor promotion of Teleocidin, even at the dose atwhich Staurosporine itself induced tumors 3. Staurosponne (0.05 and 0.1 mg/kg intraperitoneal) attenuatesthe impaired perlormance of water maze and passive avoidance tasks, even though the drug administrationbe

9、gan 2 weeks after the lesion. Moreover, Staurosporine (0.1 mg/kg) partially reversed the decrease ofcholine acetyltransferase activity in the fronto-parietal cortex induced by basal forebrain-lesion. These resultssuggest that Staurosporine attenuates impairment of learning through reversal of damage

10、 to cholinergicneurons induced by basal forebrain-lesion 4.PROTOCOL2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEAnimal Mice 3Administration 34 Female CD-I mice are used. Various amounts of Staurosporine in 10 L of acetone are applied to the ears of8-wk-old CD-I mice. The extent of irritation is

11、expressed as the minimum dose of the compound causingirritation. Induction of HOC in Mouse Skin Staurosporine in 0.1 mL of acetone is applied to the skin of thebacks of CD-I mice, and a crude enzyme extract is obtained from the skin 18 h later. HDC activity isexpressed as pmol of CO2 released per mg

12、 of protein per l h of incubation. Induction of ODC in Mouse SkinStaurosporine in 0.2 mL of acetone is applied to the skin of the backs of CD-I mice. After 4 h, a crude enzymeextract is prepared from the epidermis, and its ODC activity is measured. Enzyme activity is expressed asnmol of CO2 per mg o

13、f protein per 30 min of incubation.Rats 4Male Kbl Wistar rats(weighing 270 to 310 g) are used. In the group which is given Staurosporine for 2 weeks,the water maze task and Staurosporine administration are started 2 weeks after the BF-lesion, and thepassive avoidance task is carried out 4 weeks afte

14、r the BFlesion. The rat received Staurosporine at doses of0.01, 0.03, 0.1, and 0.3 mg/kg (i.p., N=10 in each group for 2 weeks) 30 mm prior to the water maze trainingsessions and the passive avoidance task acquisitiontrial. In the group which is given Staurosporine for 4weeks, the drug is first give

15、n 2 weeks after the BF-lesion. The water maze task is carried out 4 weeks afterthe BF-lesion. The passive avoidance task is carried out 6 weeks after the BF-lesion. The rat receivedStaurosporine at 0.05, 0.1, and 0.2 mg/kg (i.p., N=10 in each group) once a day for 2 weeks before training,and for 2 w

16、eeks after the water maze training sessions and the passive avoidance task acquisition trial.Staurosporine is suspended in 0.3% of sodium carboxymethyl cellulose. The vehicle is administered to thenon-lesioned controls and the lesioned controls on the same schedule as the Staurosporine-treated anima

17、ls.MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell. 2018 Sep 6;174(6):1477-1491.e19. J Am Chem Soc. 2018 Feb 7;140(5):1863-1869. Autophagy. 2019 Nov;15(11):1990-2001. Cancer Res. 2013 Apr 15;73(8):2574-86. J Colloid Interface Sci. 2019 May 1;543:9

18、6-105.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Meggio F, et al. Different susceptibility of protein kinases to staurosporine inhibition. Kinetic studies and molecular bases for theresistance of protein kinase CK2. Eur J Biochem. 1995 Nov 15;234(1):317-22.2. Chae HJ, et al. Molecular mechanism of staurosporine-induced apoptosis in osteoblasts. Pharmacol Res. 2000 Oct;42(4):373-81.