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Rottlerin (CAS 82-08-6)

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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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Product NameCatalog #UnitPriceQtyAddFavorites
Rottlerin sc-3550 10 mg $57
Rottlerin sc-3550A 50 mg $240
Description
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.
Technical Information
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
Density:1.36 g/cm3
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
Safety and Reference Information
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
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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
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