Rottlerin (Synonyms: Mallotoxin, NSC 94525, NSC 56346) |
| رقم الكتالوجGC10820 |
Rottlerin ، منتج طبيعي منقى من Mallotus Philippinensis ، هو مثبط محدد لـ PKC ، مع قيم IC50 لـ PKCδ من 3-6 ميكرومتر ، PKCα ، β ، من 30-42 ميكرومتر ، PKCε ، η ، ζ 80-100 ميكرومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1982/8/6
Sample solution is provided at 25 µL, 10mM.
Rottlerin was originally identified as an inhibitor of PKCδ (IC50 = 3 μM), but can also inhibit CAM kinase III and a wide range of protein kinases, including PRAK and MAPKAP-K2 (IC50s = 1.9 and 5 μM, respectively).[1],[2] It can act as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1.[3] Rottlerin has also been shown to have neuroprotective effects in an MPTP animal model of Parkinson’s disease.[4]
Reference:
[1]. McGovern, S.L., and Shoichet, B.K. Kinase inhibitors: Not just for kinases anymore Journal of Medicinal Chemistry 46, 1478-1483 (2003).
[2]. Davies, S.P., Reddy, H., Caivano, M., et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors Biochem. J. 351(1), 95-105 (2000).
[3]. Balgi, A.D., Fonseca, B.D., Donohue, E., et al. Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling PLoS One 4(9), 1-15 (2009).
[4]. Zhang, D., Anantharam, V., Kanthasamy, A., et al. Neuroprotective effect of protein kinase Cδ inhibitor rottlerin in cell culture and animal models of Parkinson’s disease Journal of Pharmacology and Experimental Therapeutics 322(3), 913-922 (2007).
| Cell experiment [1,2]: | |
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Cell lines |
Rat (C6) and two human gliomas (T98G and U138MG), glial cells, Rat lung microvascular endothelial cells, Rat primary pulmonary artery endothelial cells |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
24 h |
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Applications |
Rottlerin (24 h) decreased the growth of C6, T98G, and U138MG cells (IC50, 12 μM for C6 and >20 μM for T98G and Ui 38MG, respectively). Rottlerin (48 h) decreased the growth of C6, T98G, and Ui 38MG cells with the IC50 of 5, 7, and 9 μM, respectively. Rottlerin (5 μM) significantly reduced the number of S-phase cells in C6, T98G, and U138MG. In C6 cells, rottlerin treatment resulted in an accumulation of cytoplasmic vacuoles and packaging of cellular components within membranes. Rottlerin (5 μM) produced obvious DNA laddering in HL-60 human leukemia cells. Rottlerin dose-dependently increased basal endothelial monolayer permeability in rat LMVEC and PAEC. Rottlerin caused actomyosin filament and focal adhesion disruption. |
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References: [1]. Parmer T G, Ward M D, Hait W N. Effects of rottlerin, an inhibitor of calmodulin-dependent protein kinase III, on cellular proliferation, viability, and cell cycle distribution in malignant glioma cells[J]. Cell growth & differentiation: the molecular biology journal of the American Association for Cancer Research, 1997, 8(3): 327-334. |
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| Cas No. | 1982/8/6 | SDF | |
| المرادفات | Mallotoxin, NSC 94525, NSC 56346 | ||
| Chemical Name | (Z)-1-(6-(3-acetyl-2,4,6-trihydroxy-5-methylbenzyl)-5,7-dihydroxy-2,2-dimethyl-2H-chromen-8-yl)-3-phenylprop-2-en-1-one | ||
| Canonical SMILES | OC1=C2C(OC(C)(C)C=C2)=C(C(/C=C\C3=CC=CC=C3)=O)C(O)=C1CC(C(O)=C(C)C(O)=C4C(C)=O)=C4O | ||
| Formula | C30H28O8 | M.Wt | 516.55 |
| الذوبان | >12.5mg/mL in DMSO (ultrasonic and warming and heat to 60°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9359 mL | 9.6796 mL | 19.3592 mL |
| 5 mM | 0.3872 mL | 1.9359 mL | 3.8718 mL |
| 10 mM | 0.1936 mL | 0.968 mL | 1.9359 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)
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