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Rottlerin

PKCδ inhibitor
 
ALX-350-075-M010 10 mg 57.00 USD
 
ALX-350-075-M025 25 mg 124.00 USD
 
Replaces Prod. #: BML-EI270

Mitochondrial uncoupler that depolarizes the mitochondrial membrane potential, reduces cellular ATP levels, activates 5‘-AMP-activated protein kinase (AMPK) and affects mitochondrial production of reactive oxygen species (ROS). Potent activator of multiple Ca2+-sensitive K+ channels. Blocks several kinases and non-kinase proteins in vitro. Has been widely-used as a selective inhibitor of protein kinase Cδ (PKCδ) (IC50=3-6µM). Although there is extensive published documentation to support the use of rottlerin as a selective PKCδ inhibitor, there has been some controversy in the literature over this claim. Some of this controversy may arise from the fact that rottlerin is a promiscuous inhibitor and therefore may not always display the same properties as would be expected from a classical 1:1 inhibitor. However, there are studies indicate that rottlerin has no direct effect on PKCδ and that it should not be used to determine the involvement of PKCδ in biological processes. Induces autophagy by inhibition of mTORC1 signaling.

Product Specification

Alternative Name:Mallotoxin
 
Formula:C30H28O8
 
MW:516.5
 
Source:Isolated from Mallotus philippinensis.
 
CAS:82-08-6
 
MI:14: 8272
 
RTECS:AM6913800
 
Purity:≥98% (TLC)
 
Appearance:Orange to brown solid.
 
Solubility:Soluble in DMSO (up to 50mg/ml).
 
Long Term Storage:Ambient
 
ALX-350-075
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ALX-350-075

Product Literature References

Screen for Chemical Modulators of Autophagy Reveals Novel Therapeutic Inhibitors of mTORC1 Signaling: A.D. Balgi, et al.; PLOS ONE 4, e7124 (2009), Abstract;
Rottlerin induces autophagy and apoptotic cell death through a PKC-delta-independent pathway in HT1080 human fibrosarcoma cells: the protective role of autophagy in apoptosis: K.S. Song, et al.; Autophagy 4, 650 (2008), Abstract;
Rottlerin: an inappropriate and ineffective inhibitor of PKCdelta: S.P. Soltoff; TIPS 28, 453 (2007), Abstract;
Effect of detergent on "promiscuous" inhibitors: A.J. Ryan, et al.; J. Med. Chem. 46, 3448 (2003), Abstract;
Elongation factor-2 kinase: effective inhibition by the novel protein kinase inhibitor rottlerin and relative insensitivity towards staurosporine: M. Gschwendt, et al.; FEBS Lett. 338, 85 (1994), Abstract;
Rottlerin, a novel protein kinase inhibitor: M. Gschwendt, et al.; BBRC 199, 93 (1994), Abstract;
The mouse ear edema: a quantitatively evaluable assay for tumor promoting compounds and for inhibitors of tumor promotion: M. Gschwendt, et al.; Cancer Lett. 25, 177 (1984), Abstract;

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