Rottlerin Rottlerin is an inhibitor of eEF2K, PKCδ, PKCα, PKCβ, PKCε, PKCη and PKCζ, but with significantly reduced potency. It is also a HERG activator.

Rottlerin  (CAS 82-08-6)

Rottlerin is rated 5.0 out of 5 by 2.
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| See 11 Citations
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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Ordering Information

PRODUCT NAME CATALOG # UNIT PRICE QTY FAVORITES
Rottlerin sc-3550 10 mg $57.00
Rottlerin sc-3550A 50 mg $254.00

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
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
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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Certificate of Analysis

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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 11 total

PMID: # 25827954
Gonnella, R. et al. 2015. PKC theta and p38 MAPK activate the EBV lytic cycle through autophagy induction. Biochim. Biophys. Acta. 1853: 1586-95.

PMID: # 25355318
Wang, Y. et al. 2014. p32 is a novel target for viral protein ICP34.5 of herpes simplex virus type 1 and facilitates viral nuclear egress. The Journal of biological chemistry. 289: 35795-805.

PMID: # 25355318
Wang, Y. et al. 2014. p32 is a novel target for viral protein ICP34.5 of herpes simplex virus type 1 and facilitates viral nuclear egress. J. Biol. Chem.. 289: 35795-805.

PMID: # 22209005
Ku, CS. et al. 2012. Unsaturated fatty acids repress expression of ATP binding cassette transporter A1 and G1 in RAW 264.7 macrophages. J. Nutr. Biochem.. 23: 1271-6.

PMID: # 21530801
Ku, CS. et al. 2011. Unsaturated fatty acids repress the expression of ATP-binding cassette transporter A1 in HepG2 and FHs 74 Int cells. Nutr Res. 31: 278-85.

PMID: # 20674954
Leach, NR. et al. 2010. Significance of host cell kinases in herpes simplex virus type 1 egress and lamin-associated protein disassembly from the nuclear lamina. Virology. 406: 127-37.

PMID: # 19295663
Wang, F. et al. 2009. Role of protein kinase C beta2 activation in TNF-alpha-induced human vascular endothelial cell apoptosis. Can. J. Physiol. Pharmacol.. 87: 221-9.

PMID: # 18374649
Perissi, V. et al. 2008. TBL1 and TBLR1 phosphorylation on regulated gene promoters overcomes dual CtBP and NCoR/SMRT transcriptional repression checkpoints Molecular Cell. 29: 755-766.

PMID: # 16364465
Tapia, JA. et al. 2006. Rottlerin inhibits stimulated enzymatic secretion and several intracellular signaling transduction pathways in pancreatic acinar cells by a non-PKC-delta-dependent mechanism. Biochim. Biophys. Acta. 1763: 25-38.

PMID: # 12941843
Tillman, DM. et al. 2003. Rottlerin sensitizes colon carcinoma cells to tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis via uncoupling of the mitochondria independent of protein kinase C. Cancer Res.. 63: 5118-5125.

Citations 1 to 10 of 11 total
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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
Rated 5 out of 5 by from No comment No comment
Date published: 2015-03-31
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