Sotrastaurin

Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively[1].

Product Specifications

CAS Number

[425637-18-9]

Product Name Alternative

AEB071

UNSPSC

12352005

Hazard Statement

H301, H311, H331, H341

Target

MARCKS; PKC

Type

Reference compound

Related Pathways

Cytoskeleton; Epigenetics; TGF-beta/Smad

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Cancer

Assay Protocol

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

Purity

99.79

Solubility

DMSO : ≥ 50 mg/mL

Smiles

O=C(C(C1=C2C=CC=CC2=NC(N3CCN(C)CC3)=N1)=C4C5=CNC6=C5C=CC=C6)NC4=O

Molecular Formula

C25H22N6O2

Molecular Weight

438.48

Precautions

H301, H311, H331, H341

References & Citations

[1]Evenou JP, et al. The potent protein kinase C-selective inhibitor AEB071 (sotrastaurin) represents a new class of immunosuppressive agents affecting early T-cell activation. J Pharmacol Exp Ther. 2009 Sep;330 (3) :792-801.|[2]Musi E, et al. The phosphoinositide 3-kinase α selective inhibitor BYL719 enhances the effect of the protein kinase C inhibitor AEB071 in GNAQ/GNA11-mutant uveal melanoma cells. Mol Cancer Ther. 2014 May;13 (5) :1044-53|[3]Kamo N, et al. Sotrastaurin, a protein kinase C inhibitor, ameliorates ischemia and reperfusion injury in rat orthotopic liver transplantation. Am J Transplant. 2011 Nov;11 (11) :2499-507.