KUN79359

KUN79359, also known as RIP1 kinase inhibitor and PKCß inhibitor, is a potent and selective inhibitor of PKCß isozymes.

Product information

CAS Number: 257879-35-9

Molecular Weight: 411.46

Formula: C24H21N5O2

Synonym:

PKCß inhibitor

RIP1 kinase inhibitor

KUN-79359

KUN79359

Chemical Name:  3-[1-(3-Imidazol-1-yl-propyl)-1H-indol-3-yl]-4-phenylamino-pyrrole-2,5-dione

Smiles: O=C1NC(=O)C(NC2C=CC=CC=2)=C1C1=CN(CCCN2C=NC=C2)C2=CC=CC=C21

InChiKey: KIWODJBCHRADND-UHFFFAOYSA-N

InChi: InChI=1S/C24H21N5O2/c30-23-21(22(24(31)27-23)26-17-7-2-1-3-8-17)19-15-29(20-10-5-4-9-18(19)20)13-6-12-28-14-11-25-16-28/h1-5,7-11,14-16H,6,12-13H2,(H2,26,27,30,31)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

KUN79359 (0-30 μM; 48 hours) suppresses tumor cell proliferation in a time- and dose-dependent manner. KUN79359 (14 μM; 2-48 hours) induces apoptosis in 2F7 cells. KUN79359 (15 μM; 2-48 hours) inhibits cell cycle progression in 2F7 and BCBL-1 cells. KUN79359 (15 or 14 μM, respectively; 2-48 hours) inhibitor 1 reduces the expression of phospho-PKCβ in BCBL-1 and 2F7 cells. KUN79359 (0-48 hours) suppresses GSK3β, mTOR, and S6 phosphorylation.

References:

1. Pakhomov N, Pustovit K, Potekhina V, Filatova T, Kuzmin V, Abramochkin D. Negative inotropic effects of diadenosine tetraphosphate are mediated by protein kinase C and phosphodiesterases stimulation in the rat heart. Eur J Pharmacol. 2017 Dec 9. pii: S0014-2999(17)30818-X. doi: 10.1016/j.ejphar.2017.12.024. [Epub ahead of print] PubMed PMID: 29233660.
2. Campana M, Bellini L, Rouch C, Rachdi L, Coant N, Butin N, Bandet CL, Philippe E, Meneyrol K, Kassis N, Dairou J, Hajduch E, Colsch B, Magnan C, Le Stunff H. Inhibition of central de novo ceramide synthesis restores insulin signaling in hypothalamus and enhances β-cell function of obese Zucker rats. Mol Metab. 2017 Nov 7. pii: S2212-8778(17)30690-7. doi: 10.1016/j.molmet.2017.10.013. [Epub ahead of print] PubMed PMID: 29233519.
3. Lu T, Chou CT, Liang WZ, Kuo CC, Chen IL, Wang JL, Jan CR. Amitriptyline modulated Ca(2+) signaling and induced Ca(2+)-independent cell viability in human osteosarcoma cells. Hum Exp Toxicol. 2017 Jan 1:960327117693070. doi: 10.1177/0960327117693070. [Epub ahead of print] PubMed PMID: 29233021.

Products are for research use only. Not for human use.