Rottlerin

- Overview
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    Background
    
    Rottlerin is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM[1].
    Rottlerin (20 μM, 2/6/24 hours) dramatically decreases the cyclin D-1 mRNA levels in a time-dependent manner and exhibits cell proliferation in HMVEC[2].
    In Balb C nude mice, rottlerin (20 mg/kg, gavage 5 days per week, once daily, for 6 weeks) inhibits AsPC-1 pancreatic tumor growth with no toxicity. Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP)[3].
    
    [1]. Gschwendt M, et al. Rottlerin, a novel protein kinase inhibitor. Biochem Biophys Res Commun, 1994, 199(1): 93-8.
    [2]. Valacchi G, et al. Rottlerin exhibits antiangiogenic effects in vitro. Chem Biol Drug Des, 2011, 77(6): 460-70.
    [3]. Minzhao Huang, et al. Rottlerin suppresses growth of human pancreatic tumors in nude mice, and pancreatic cancer cells isolated from KrasG12D mice. Cancer Letters, 2014, 353(1): 32-40.
- Properties
  - Alternative 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
    
    CAS Number
    
    82-08-6
    
    Molecular Formula
    
    C30H28O8
    
    Molecular Weight
    
    516.55
    
    Appearance
    
    A yellow to orange solid
    
    Purity
    
    Purity ≥90.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥23.6 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Dong Y, Gao J, et al. "Antigen-Conjugated Silica Solid Sphere as Nanovaccine for Cancer Immunotherapy." Int J Nanomedicine. 2020;15:2685-2697. PMID:32368049
    2. Wei P, Ning M, et al. "Spiroplasma eriocheiris entered Drosophila Schneider 2 cells and relied on clathrin-mediated endocytosis and macropinocytosis." Infect Immun. 2019 Aug 26. pii: IAI.00233-19. PMID:31451616
    3. Wang H, Liu W, et al. "Inhibitor analysis revealed that clathrin-mediated endocytosis is involed in cellular entry of type III grass carp reovirus." Virol J. 2018 May 24;15(1):92. PMID:29793525

Rottlerin

Background

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