82-08-6 Usage
Description
Rottlerin is a naturally occurring compound extracted from Mallotus philippinensis, characterized by its unique chemical structure as a chromenol with specific substitutions. It has been reported to inhibit protein kinase Cδ (PKCδ) selectively, although this has been debated. Rottlerin also functions as a human ether-a-go-go-related gene (hERG) potassium channel activator, an uncoupler of mitochondrial respiration, and exhibits neuroprotective effects, inducing autophagy and possessing cell permeability. It is known for its antitumor, anti-proliferative, anti-metastasis, and anti-invasive properties.
Uses
Used in Pharmaceutical and Biomedical Research:
Rottlerin is used as a research tool for studying the role of PKCδ in various cellular processes due to its reported inhibitory effects on this enzyme. Its potential in modulating cellular functions makes it valuable in understanding the underlying mechanisms of diseases and developing therapeutic strategies.
Used in Cancer Therapy Research:
Rottlerin is used as an antitumor agent in cancer research, targeting multiple aspects of cancer progression, including proliferation, metastasis, and invasion. Its multifaceted action against cancer cells highlights its potential in developing novel cancer treatments.
Used in Neuroprotective Studies:
Given its neuroprotective effects, Rottlerin is used in research aimed at understanding and treating neurodegenerative diseases and conditions where neuronal protection and survival are critical.
Used in Autophagy Research:
Rottlerin's ability to induce autophagy makes it a useful compound in studying the process of autophagy, which is essential for maintaining cellular homeostasis and has implications in various diseases, including cancer and neurodegenerative disorders.
Used in Mitochondrial Function Studies:
As an uncoupler of mitochondrial respiration from oxidative phosphorylation, Rottlerin is utilized in research to investigate the relationship between mitochondrial function and various physiological and pathological conditions.
Biological Activity
Originally reported to inhibit PKC isoforms, with selectivity for PKC δ (K i values are 30, 42, 40, 3-6, 100, and 100 μ M for α , β , γ , δ , ε , λ respectively). Also reported to inhibit CAM kinase III. However, recently shown to inhibit a wide range of protein kinases, and most potently to inhibit PRAK and MAPKAP-K2 (IC 50 values are 1.9 and 5 μ M respectively). Also shown to act as a direct mitochondrial uncoupler.
Biochem/physiol Actions
Recently, Rottlerin (mallotoxin) has been shown to be a potent activator of the large conductance voltage and Ca2 activated K+ channel and to potently leftward shift the conductance-voltage relationship of the channel. Mallatoxin tested on hERG channels increased both step and tail hERG current by leftward shifting the voltage dependence of hERG activation and slowing channel deactivation. These actions distinguish Mallatoxin as a novel naturally occurring hERG channel activator.
References
1) Davies et al. (2000), Specificity and mechanism of action of some commonly used protein kinase inhibitors; Biochem. J., 351 95
2) Zhang et al. (2007), Neuroprotective effect of protein kinase C delta inhibitor rottlerin in cell culture and animal models of Parkinson’s disease; J. Pharmacol. Exp. Ther., 322 913
3) Balgi et al. (2009), Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling; PLoS One, 4 e7124
Check Digit Verification of cas no
The CAS Registry Mumber 82-08-6 includes 5 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 2 digits, 8 and 2 respectively; the second part has 2 digits, 0 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 82-08:
(4*8)+(3*2)+(2*0)+(1*8)=46
46 % 10 = 6
So 82-08-6 is a valid CAS Registry Number.
InChI:InChI=1/C30H28O8/c1-15-24(33)19(27(36)22(16(2)31)25(15)34)14-20-26(35)18-12-13-30(3,4)38-29(18)23(28(20)37)21(32)11-10-17-8-6-5-7-9-17/h5-13,33-37H,14H2,1-4H3/b11-10+
