RottlerinA widely-used selective inhibitor of PKCδ

Rottlerin (CAS 82-08-6)

Rottlerin | CAS 82-08-6 is rated 5.0 out of 5 by 2.
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Synonym: Mallotoxin
Application: A widely-used selective inhibitor of PKCδ
CAS Number: 82-08-6
Purity: ≥98%
Molecular Weight: 516.54
Molecular Formula: C30H28O8
* Refer to Certificate of Analysis for lot specific data (including water content).
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Rottlerin is a principal phenolic compound of the Kamala plant Mallotus philippinensis. It is a widely-used selective inhibitor of PKCδ (protein kinase Cδ) (IC50=3-6 μM). It also inhibits PKCα, PKCβ, PKCγ, PKCε, PKCη, PKCζ and eEF2K (CaMK III) (IC50 = 5.3 μM). In HT1080 human fibrosarcoma cells, rottlerin induces apoptosis and autophagy via a PKCδ-independent pathway. When tested on HERG (human Ether-á-go-go) channels, rottlerin increased both step and tail HERG current by leftward shifting the voltage and dependence of HERG activation and slowing channel deactivation. Rottlerin is an inhibitor of Chk2, MAPKAPK-2, Pim-3, PKCλ, PKCθ, Plk, PRAK, SRPK1 and an activator of AMPK and HERG. There have been a number of studies published with evidence against the role of Rotterlin as a specific PKCδ inhibitor.


References

1. Gschwendt, M., et al. 1984. Cancer Lett. 25: 177-185. PMID: 6509437
2. Gschwendt, M., et al. 1994. Biochem. Biophys. Res. Commun. 199: 93-98. PMID: 8123051
3. Gschwendt, M., et al. 1994. FEBS Lett. 338: 85-88. PMID: 8307162
4. Zeng, H., et al. 2006. J. Pharmacol. Exp. Ther. 319: 957-962. PMID: 16928897
5. Song, K.S., et al. 2008. Autophagy. 4: 650-658. PMID: 18424913
6. Balgi, A.D., et al. 2009. PLoS ONE. 4: e7124. PMID: 19771169
7. Yin, S., et al. 2010. J Cell Biochem. PMID: 20665667

Physical State :
Solid
Derived From :
Mallotus philippinensis
Solubility :
Soluble in ethanol (1 mg/ml), DMSO (30 mg/ml), DMF, ether, chloroform, benzene, and ethyl acetate. Insoluble in water.
Storage :
Store at -20° C
Melting Point :
>200° C
Boiling Point :
~800.44° C at 760 mmHg (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.68
IC50 :
PKCδ: IC50 = 3-6 µM; PKCα: IC50 = 30-42 µM; PKCβ: IC50 = 30-42 µM; PKCγ: IC50 = 30-42 µM; PKCε: IC50 = 80-100 µM; PKCη: IC50 = 80-100 µM; PKCζ: IC50 = 80-100 µM; PRAK: IC50 = 1.9 µM; MAPKAP-K2: IC50 = 5 µM; CaM kinase III: IC50 = 5.3 µM
Ki Data :
PKCα: Ki= 30 µM; PKCβ: Ki= 42 µM; PKCγ: Ki= 40 µM; PKCδ: Ki= 3-6 µM; PKCε: Ki= 100 µM; PKCλ: Ki= 100 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
AM6913800
PubChem CID :
5281847
Merck Index :
14: 8272
MDL Number :
MFCD00017361
EC Number :
201-395-4
SMILES :
CC1=C(C(=C(C(=C1O)C(=O)C)O)CC2=C(C3=C(C(=C2O)C(=O)/C=C/C4=CC=CC=C4)OC(C=C3)(C)C)O)O

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Rottlerin  Product Citations

See how others have used Rottlerin. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 27 total

PMID: # 30982662  Moreau, HD. et al. 2019. Dev. Cell. 49: 171-188.e5.

PMID: # 30168902  Liu, L. et al. 2018. Cancer Sci. 109: 3611-3622.

PMID: # 29522984  Wang, R. et al. 2018. Virology. 518: 172-183.

PMID: # 28801242  Gonnella, R. et al. 2017. Free Radic. Biol. Med. 112: 327-335.

PMID: # 29383184  Lee, KH. et al. 2017. Oncotarget. 8: 115596-115608.

PMID: # 28983628  Zhou, T. et al. 2017. Mol Med Rep. 16: 8513-8519.

PMID: # 27667474  Yang, T. et al. 2017. Endocr. J. 64: 15-26.

PMID: # 26995094  Zielinski, J. et al. 2016. Nanomedicine. 12: 1603-13.

PMID: # 27313531  Xiao, F. et al. 2016. Front Pharmacol. 7: 146.

PMID: # 27889758  Mischitelli, M. et al. 2016. Cell. Physiol. Biochem. 40: 558-566.

Citations 1 to 10 of 27 total
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Rated 5 out of 5 by from No comment No comment
Date published: 2015-03-31
Rated 5 out of 5 by from Rottlerin Rottlerin, a PKC inhibitor purchased from SCBT, was used to eliminate the epitope specifically recognized by the Mono-P-TBLR1 antibody (PubMed ID 18374649). -SCBT Publication Review
Date published: 2015-03-31
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