Rottlerin

Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα, β, γ of 30-42 μM, PKCε, η, ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation[1][2][3]. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection[4][5].

Product Specifications

CAS Number

[82-08-6]

Product Name Alternative

Mallotoxin; NSC 56346; NSC 94525

UNSPSC

12352005

Hazard Statement

H302+H312+H332, H315, H319, H335

Target

Apoptosis; Autophagy; HIV; PKC; RABV

Type

Natural Products

Related Pathways

Anti-infection; Apoptosis; Autophagy; Epigenetics; TGF-beta/Smad

Applications

COVID-19-immunoregulation

Field of Research

Infection; Cancer

Assay Protocol

https://www.medchemexpress.com/Rottlerin.html

Concentration

10mM

Purity

98.45

Solubility

DMSO : 12.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1=C2C(C=CC(C)(C)O2)=C(O)C(CC3=C(O)C(C)=C(O)C(C(C)=O)=C3O)=C1O)/C=C/C4=CC=CC=C4

Molecular Formula

C30H28O8

Molecular Weight

516.54

Precautions

H302+H312+H332, H315, H319, H335

References & Citations

[1]Gschwendt M, et al. Rottlerin, a novel protein kinase inhibitor. Biochem Biophys Res Commun. 1994 Feb 28;199 (1) :93-8.|[2]Valacchi G, et al. Rottlerin exhibits antiangiogenic effects in vitro. Chem Biol Drug Des. 2011 Jun;77 (6) :460-70.|[3]Minzhao Huang, et al. Rottlerin suppresses growth of human pancreatic tumors in nude mice, and pancreatic cancer cells isolated from KrasG12D mice. Cancer Letters 353 (2014) 32-40.|[4]María Rosa López-Huertas, et al. Protein kinase Ctheta is a specific target for inhibition of the HIV type 1 replication in CD4+ T lymphocytes. J Biol Chem. 2011 Aug 5;286 (31) :27363-77.|[5]Zoé Lama, et al. Kinase inhibitors tyrphostin 9 and rottlerin block early steps of rabies virus cycle. Antiviral Res. 2019 Aug;168:51-60.