An inhibitor of PKCδ and other protein kinases
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Rottlerin

Item No. 12006

Technical Information
Formal Name
(2E)-1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-8-yl]-3-phenyl-2-propen-1-one
CAS Number
82-08-6
Synonyms
  • Mallotoxin
  • NSC 94525
  • NSC 56346
Molecular Formula
C30H28O8
Formula Weight
Purity
≥95%
A solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: 1.25 mg/ml
SMILES
OC1=C(C)C(O)=C(C(C)=O)C(O)=C1CC2=C(O)C(C=CC(C)(C)O3)=C3C(C(/C=C/C4=CC=CC=C4)=O)=C2O
InChi Code
InChI=1S/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+
InChi Key
DEZFNHCVIZBHBI-ZHACJKMWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Rottlerin was originally identified as an inhibitor of PKCδ (IC50 = 3 μM), but can also inhibit CAM kinase III and a wide range of protein kinases, including PRAK and MAPKAP-K2 (IC50s = 1.9 and 5 μM, respectively).1,2 It can act as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1.3 Rottlerin has also been shown to have neuroprotective effects in an MPTP animal model of Parkinson’s disease.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. McGovern, S.L., and Shoichet, B.K. Kinase inhibitors: Not just for kinases anymore. J. Med. Chem. 46(8), 1478-1483 (2003).

    2. Davies, S.P., Reddy, H., Caivano, M., et alSpecificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem. J. 351(1), 95-105 (2000).

    3. Balgi, A.D., Fonseca, B.D., Donohue, E., et alScreen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling. PLoS One 4(9), e7124 (2009).

    4. Zhang, D., Anantharam, V., Kanthasamy, A., et alNeuroprotective effect of protein kinase Cδ inhibitor rottlerin in cell culture and animal models of Parkinson’s disease. J. Pharmacol. Exp. Ther. 322(3), 913-922 (2007).