KIRA6_product_DataBase

Bioactivity

KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC50 of 0.6 µM[2]. KIRA6 can trigger an apoptotic response[1].

Target

IC50: 0.6 µM (IRE1α RNase kinase)

Invitro

KIRA6 (1nM-100μM) bounds to the cytoplasmic domain of KIT with a Kd value of 10.8 µM[1].KIRA6 (10-1000 nM; 72 hours) strongly compromises the viability of the KIT-dependent cell line HMC-1.1 at the low nM concentration, in a manner that coincided with KIT blockade[1].KIRA6 (10-1000 nM; 1 hour) reduces signaling output of KIT, including the phosphorylation of KIT as well as its downstream signaling modules, PSTAT5 and phosphorylated ERK1/2[1].KIRA6 (1 μM; 0-48 hours) inhibits Ins1 mRNA decay from IRE1α hyperactivation at a dose-dependent manner[2].KIRA6 (0.1-10μM; 72 hours) dose-dependently reduces 1NM-PP1 potentiation of Ins1 apoptosis during ER stress in a dose-dependent manner[2]. Cell Viability Assay[1] Cell Line:

In Vivo

KIRA6 (intraperitoneal injection; 5 mg/kg; 37 days) shows significant amelioration of random glucose levels over several weeks compared to vehicle, both fed ad lib[2].KIRA6 (intraperitoneal injection; 5 mg/kg; 21 or 18 days postinjections) increases both plasma insulin and C-peptide levels, remains insulin-positive islet areas at high level after stopping injections in the Akita Mouse[2]. Animal Model:

Name

KIRA6

CAS

1589527-65-0

Formula

C28H25F3N6O

Molar Mass

518.53

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Mahameed M,et al. The unfolded protein response modulators GSK2606414 and KIRA6 are potent KIT inhibitors. Cell Death Dis. 2019 Apr 1;10(4):300. [2]. Ghosh R, et al. Allosteric inhibition of the IRE1α RNase preserves cell viability and function during endoplasmic reticulum stress. Cell. 2014 Jul 31;158(3):534-48.

PeptideDB

KIRA6

CAS: 1589527-65-0 F: C28H25F3N6O W: 518.53