Rottlerin-Mallotoxin-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERottlerinCat. No.: HY-18980CAS No.: 82-08-6Synonyms: Mallotoxin; NSC 56346; NSC 94525分式: CHO分量: 516.54作靶点: PKC; Autophagy; Apoptosis作通路: Epigenetics; TGF-beta/Smad; Autophagy; Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solven

2、t -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 2 mg/mL (3.87 mM; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.9360 mL 9.6798 mL 19.3596 mL5 mM - - -10 mM - - -请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Rottlerin可从Mallotus Philip

3、pinensis中的到的种天然产物， PKC 的个特异性抑制剂，其对 PKC的 IC50 值为 3-6 M， PKC, 的为 30-42 M，PKC, 为 80-100 M。Rottlerin 可作为线粒体直接解偶联剂，通过编写那个mTOR1上游的信号级联刺激噬。Rottlerin 通过活化caspase 3诱导细胞凋亡。IC50 & Target PKC PKC PKC PKC1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3 M (IC50, Porcine 30 M (IC50, 40 M (IC50, 42 M (IC50,spleen

4、) baculovirus-infected baculovirus-infected baculovirus-infectedSf9 insect cells) Sf9 insect cells) Sf9 insect cells)PKC PKC PKC CaM kinase III82 M (IC50, 100 M (IC50, 100 M (IC50, 5.3 M (IC50, EF-2baculovirus-infected Sf9 baculovirus-infected baculovirus-infected kinase activity ininsect cells) Sf9

5、 insect cells) Sf9 insect cells) cytosol of murinepancreas)CKII PKA30 M (IC50, 78 M (IC50, catalyticholoenzyme expressed subunit from porcinein E.coli) heart)体外研究 Rottlerin (20 M, 2/6/24 hours) dramatically decreases the cyclin D-1 mRNA levels in a time-dependentmanner in primary HMVEC 2.Rottlerin (

6、20 M) exhibits cell proliferation in HMVEC 2.Western Blot Analysis 2Cell Line: Primary HMVEC (Human Microvascular Endothelial Cell).Concentration: 20 M.Incubation Time: 2, 6, 24 hours.Result: Dramatically decreased the cyclin D-1 mRNA levels in a time-dependent manner. After 2h of treatment, the mRN

7、A level was reduced to 50% of the control, to circa 40% after 6 h,and to 20% after 24 h. Consistently, a similar trend was observed in the protein levels,where the decrease was circa 50% after 2 h, 80% after 6 h, and to almost undetectablelevels after 24 h.Cell Proliferation Assay 2Cell Line: Primar

8、y HMVEC (Human Microvascular Endothelial Cell).Concentration: 20 M.Incubation Time: 24/48 hours.Result: Exhibited a strong growth inhibition, with a reduction in thymidine incorporation respect tothe control cells (DMSO 0.1%) of circa 75% and 80%, respectively.体内研究Rottlerin (20 mg/kg, gavage 5 days

9、per week, once daily, for 6 weeks) inhibits AsPC-1 pancreatic tumorgrowth in Balb C nude mice with no toxicity 3.Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEof poly(ADP-ribose) polymer

10、ase (PARP) 3.Animal Model: Balb C nude mice (4-6 weeks old) with AsPC-1 cells (2106 cells mixed with Matrigel,50:50 ratio) injection 3.Dosage: 0 or 20 mg/kg.Administration: Gavage 5 days per week, once daily, for 6 weeks.Result: Inhibited AsPC-1 pancreatic tumor growth in Balb C nude mice and had no

11、 effecton thebody weight of AsPC-1 tumor-bearing mice.REFERENCES1. Gschwendt M, et al. Rottlerin, a novel protein kinase inhibitor. Biochem Biophys Res Commun. 1994 Feb 28;199(1):93-8.2. Valacchi G, et al. Rottlerin exhibits antiangiogenic effects in vitro. Chem Biol Drug Des. 2011 Jun;77(6):460-70.3. Minzhao Huang, et al. Rottlerin suppresses growth of human pancreatic tumors in nude mice, and pancreatic cancer cells isolated fromKrasG12D mice. Cancer Letters 353 (2014) 32-40.McePdfHeightCaution: Product