Rottlerin
Product Code: AG-CN2-0526
Product Group: Natural Products and Extracts
Supplier: AdipoGen Life Sciences
| Code | Size | Price |
|---|
| AG-CN2-0526-M010 | 10 mg | £55.00 |
Quantity:
| AG-CN2-0526-M050 | 50 mg | £170.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Antibody Isotype: n/a
Antibody Clone: n/a
Regulatory Status: RUO
Shipping:
Ambient
Storage:
-20°C
Documents
Further Information
Alternate Names/Synonyms:
Mallotoxin; NSC94525; NSC56346; Kamalin
Appearance:
Orange to brown solid.
CAS:
82-08-6
EClass:
32160000
Form (Short):
liquid
Handling Advice:
Keep cool and dry.
InChi:
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+
InChiKey:
DEZFNHCVIZBHBI-ZHACJKMWSA-N
Long Description:
Chemical. CAS: 82-08-6. Formula: C30H28O8. MW: 516.5. Anticancer agent that can inhibit cell growth, induce apoptosis, autophagy and cell cycle arrest, inhibit cell invasion and shows anti-angiogenic activity. OXPHOS inhibitor. Mitochondrial uncoupler that depolarizes the mitochondrial membrane potential, reduces cellular ATP levels, activates 5'-AMP-activated protein kinase (AMPK) and affects mitochondrial production of reactive oxygen species (ROS). Useful for immunometabolism research. Potent activator of multiple Ca2+-sensitive K+ channels. Naturally occurring hERG channel activator. Antioxidant and ROS scavanger. Might have cardioprotective effects. Has been widely used as a selective inhibitor of protein kinase Cdelta (PKCdelta) (IC50=3-6µM), although there has been controversy in the literature over this claim. Inhibits CAM kinase III and a wide range of other kinases and non-kinase proteins in vitro. Most potently inhibits PRAK and MAPKAP-K2. Induces autophagy by inhibition of mTORC1 signaling. Displays neuroprotective effects.
MDL:
MFCD00017361
Molecular Formula:
C30H28O8
Molecular Weight:
516.5
Package Type:
Vial
Product Description:
Anticancer agent that can inhibit cell growth, induce apoptosis, autophagy and cell cycle arrest, inhibit cell invasion and shows anti-angiogenic activity. OXPHOS inhibitor. Mitochondrial uncoupler that depolarizes the mitochondrial membrane potential, reduces cellular ATP levels, activates 5'-AMP-activated protein kinase (AMPK) and affects mitochondrial production of reactive oxygen species (ROS). Useful for immunometabolism research. Potent activator of multiple Ca2+-sensitive K+ channels. Naturally occurring hERG channel activator. Antioxidant and ROS scavanger. Might have cardioprotective effects. Has been widely used as a selective inhibitor of protein kinase Cdelta (PKCdelta) (IC50=3-6µM), although there has been controversy in the literature over this claim. Inhibits CAM kinase III and a wide range of other kinases and non-kinase proteins in vitro. Most potently inhibits PRAK and MAPKAP-K2. Induces autophagy by inhibition of mTORC1 signaling. Displays neuroprotective effects.
Purity:
>98% (HPLC)
SMILES:
CC1(C)C=CC2=C(O)C(CC3=C(O)C(C)=C(O)C(C(C)=O)=C3O)=C(O)C(C(/C=C/C4=CC=CC=C4)=O)=C2O1
Solubility Chemicals:
Soluble in DMSO (50mg/ml) or ethanol (1mg/ml). Insoluble in water.
Source / Host:
Isolated from Mallotus philippinensis.
Transportation:
Non-hazardous
UNSPSC Category:
Natural Products/Extracts
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
Rottlerin, a novel protein kinase inhibitor: M. Gschwendt, et al.; BBRC 199, 93 (1994) | Effects of rottlerin, an inhibitor of calmodulin-dependent protein kinase III, on cellular proliferation, viability, and cell cycle distribution in malignant glioma cells: T.G. Parmer, et al.; Cell Growth Differ. 8, 327 (1997) | Specificity and mechanism of action of some commonly used protein kinase inhibitors: S.P. Davies, et al.; Biochem. J. 351, 95 (2000) | Rottlerin is a mitochondrial uncoupler that decreases cellular ATP levels and indirectly blocks protein kinase Cdelta tyrosine phosphorylation: S.P. Soltoff; J. Biol. Chem. 276, 37986 (2001) | Rottlerin inhibits insulin-stimulated glucose transport in 3T3-L1 adipocytes by uncoupling mitochondrial oxidative phosphorylation: A.G. Kayali, et al.; Endocrinol. 143, 3884 (2002) | Kinase inhibitors: Not just for kinases anymore: S.L. McGovern & B.K. Shoichet; J. Med. Chem. 46, 1478 (2003) | Mitochondrial Ca2+-activated K+ channels in cardiac myocytes: a mechanism of the cardioprotective effect and modulation by protein kinase A: T. Sato, et al.; Circulation 111, 198 (2005) | Mallotoxin is a novel human ether-a-go-go-related gene (hERG) potassium channel activator: H. Zeng, et al.; JPET 319, 957 (2006) | Rottlerin: an inappropriate and ineffective inhibitor of PKCdelta: S.P. Soltoff; TIPS 28, 453 (2007) | Neuroprotective effect of protein kinase C delta inhibitor rottlerin in cell culture and animal models of Parkinson's disease: D. Zhang, et al.; J. Pharmacol. Exp. Ther. 322, 913 (2007) | Rottlerin induces autophagy and apoptotic cell death through a PKC-delta-independent pathway in HT1080 human fibrosarcoma cells: the protective role of autophagy in apoptosis: K.S. Song, et al.; Autophagy 4, 650 (2008) | Screen for Chemical Modulators of Autophagy Reveals Novel Therapeutic Inhibitors of mTORC1 Signaling: A.D. Balgi, et al.; PLOS One 4, e7124 (2009) | Rottlerin exhibits antiangiogenic effects in vitro: G. Valacchi, et al.; Chem. Biol. Drug Des. 77, 460 (2011) | Rottlerin induces autophagy and apoptosis in prostate cancer stem cells via PI3K/Akt/mTOR signaling pathway: D. Kumar, et al.; Cancer Lett. 343, 179 (2014) | Rottlerin inhibits cell growth, induces apoptosis and cell cycle arrest, and inhibits cell invasion in human hepatocellular carcinoma: J. Shi, et al.; Mol. Med. Rep. 17, 459 (2018) | Non-conventional rottlerin anticancer properties: E. Maioli, et al.; Arch. Biochem. Biophys. 645, 50 (2018)