Accéder au contenu
Merck
Toutes les photos(1)

Documents

R5648

Sigma-Aldrich

Rottlerin

Synonyme(s) :

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, Mallotoxin

Se connecterpour consulter vos tarifs contractuels et ceux de votre entreprise/organisme


About This Item

Formule empirique (notation de Hill):
C30H28O8
Numéro CAS:
Poids moléculaire :
516.54
Numéro CE :
Numéro MDL:
Code UNSPSC :
12352200
ID de substance PubChem :
Nomenclature NACRES :
NA.77

Source biologique

plant (Mallotus philippinensis)

Pureté

≥95% (HPLC)

Forme

powder

Pf

200.0 °C

Solubilité

ethanol: 1 mg/mL

Température de stockage

2-8°C

Chaîne SMILES 

CC(=O)c1c(O)c(C)c(O)c(Cc2c(O)c3C=CC(C)(C)Oc3c(c2O)C(=O)\C=C\c4ccccc4)c1O

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+

Clé InChI

DEZFNHCVIZBHBI-ZHACJKMWSA-N

Informations sur le gène

human ... CDK2(1017)

Vous recherchez des produits similaires ? Visite Guide de comparaison des produits

Description générale

Rottlerin is extracted from Mallotus philippinensis. It is a protein kinase Cδ (PKCδ) inhibitor. Rottlerin acts as an uncoupler of mitochondrial respiration from oxidative phosphorylation. It has antitumor, autophagy, anti-proliferative, anti-metastasis and anti-invasive properties.

Application

Rottlerin has been used:
  • as a protein kinase C δ (PKCδ) inhibitor for the analysis of protein content and phosphorylation in rats
  • to examine the gene expression of early osteoblast markers
  • to attenuate pyruvate dehydrogenase (PDH) phosphorylation by succinate
  • to depolarise mitochondria
  • to investigate its antitumor activity in pancreatic cancer (PC) cells

Actions biochimiques/physiologiques

Recently, Rottlerin (mallotoxin) has been shown to be a potent activator of the large conductance voltage and Ca2 activated K+ channel and to potently leftward shift the conductance-voltage relationship of the channel. Mallatoxin tested on hERG channels increased both step and tail hERG current by leftward shifting the voltage dependence of hERG activation and slowing channel deactivation. These actions distinguish Mallatoxin as a novel naturally occurring hERG channel activator.

Caractéristiques et avantages

This compound is featured on the PKC page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Code de la classe de stockage

13 - Non Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Équipement de protection individuelle

Eyeshields, Gloves, type N95 (US)


Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

Déjà en possession de ce produit ?

Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

The unfolded protein response plays a predominant homeostatic role in response to mitochondrial stress in pancreatic stellate cells
Su HY, et al.
Testing, 11(2), e0148999-e0148999 (2016)
Haoyu Zeng et al.
The Journal of pharmacology and experimental therapeutics, 319(2), 957-962 (2006-08-25)
Human ether-a-go-go-related gene (hERG) encodes a rapidly activating delayed rectifier potassium channel that plays important roles in cardiac action potential repolarization. Although many drugs and compounds block hERG channels, activators of the channel have only recently been described. Three structurally
Jui-Ling Hsu et al.
Biochemical pharmacology, 84(1), 59-67 (2012-04-12)
Combination therapy, which can optimize killing activity to cancers and minimize drug resistance, is a mainstream therapy against hormone-refractory prostate cancers (HRPCs). Rottlerin, a natural polyphenolic component, synergistically increased PC-3 (a HRPC cell line) apoptosis induced by camptothecin (a topoisomerase
Succinate accumulation impairs cardiac pyruvate dehydrogenase activity through GRP91-dependent and independent signaling pathways: Therapeutic effects of ginsenoside Rb1
Li J, et al.
Biochimica et Biophysica Acta (BBA)-Molecular Basis of Disease, 1863(11), 2835-2847 (2017)
Rottlerin exhibits antitumor activity via down-regulation of TAZ in non-small cell lung cancer
Zhao Z, et al.
Testing, 8(5), 7827-7827 (2017)

Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..

Contacter notre Service technique