KUN79359

Cas：257879-35-9

Product Information：

KUN79359, also known as RIP1 kinase inhibitor and PKCß inhibitor, is a potent and selective inhibitor of PKCß isozymes. KUN79359 has no formal name, and has CAS#257879-35-9. For the convenience of scientific communication, it is named as KUN79359. The name was generated based on Hodoodo chemical nomenclature.

Chemical Formula: C24H21N5O2

Exact Mass: 411.17

Molecular Weight: 411.46

Elemental Analysis: C, 70.06; H, 5.14; N, 17.02; O, 7.78

Related CAS #: 257879-35-9  

Synonym:

PKCß inhibitor

RIP1 kinase inhibitor

KUN79359

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

InChi Key:

KIWODJBCHRADND-UHFFFAOYSA-N

InChi Code: 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)

Smiles Code:

O=C(C(C1=CN(CCCN2C=CN=C2)C3=C1C=CC=C3)=C4NC5=CC=CC=C5)NC4=O

Technical Data：

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

In Vitro：

PKCβ inhibitor 1 (0-30 μM; 48 hours) suppresses tumor cell proliferation in a time- and dose-dependent manner.

PKCβ inhibitor 1 (14 μM; 2-48 hours) induces apoptosis in 2F7 cells.

PKCβ inhibitor 1 (15 μM; 2-48 hours) inhibits cell cycle progression in 2F7 and BCBL-1 cells.

PKCβ (15 or 14 μM, respectively; 2-48 hours) inhibitor 1 reduces the expression of phospho-PKCβ in BCBL-1 and 2F7 cells.

PKCβ inhibitor 1(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.

4. Weng Y, Mizuno N, Dong J, Segawa R, Yonezawa T, Cha BY, Woo JT, Moriya T, Hiratsuka M, Hirasawa N. Induction of thymic stromal lymphopoietin by a steroid alkaloid derivative in mouse keratinocytes. Int Immunopharmacol. 2017 Dec 5;55:28-37. doi: 10.1016/j.intimp.2017.11.045. [Epub ahead of print] PubMed PMID: 29220720.

5. Lozanoska-Ochser B, Benedetti A, Rizzo G, Marrocco V, Di Maggio R, Fiore P, Bouche M. Targeting early PKCθ-dependent T cell infiltration of dystrophic muscle reduces disease severity in a mouse model of muscular dystrophy. J Pathol. 2017 Dec 7. doi: 10.1002/path.5016. [Epub ahead of print] PubMed PMID: 29214629.

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