[CAS NO. 1589527-65-0] KIRA6

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PRODUCTS SPECIFICATIONS [1589527-65-0]

Catalog

HY-19708

Brand

MCE

CAS

1589527-65-0

DESCRIPTION [1589527-65-0]

Overview

MDL	MFCD29477497
Molecular Weight	518.53
Molecular Formula	C28H25F3N6O
SMILES	O=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=C3C=CC=CC3=C(C4=C5C(N)=NC=CN5C(C(C)(C)C)=N4)C=C2

For research use only. We do not sell to patients.

10 Publications Citing Use of MCE

Summary

KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC ₅₀ of 0.6 µM ^[2] . KIRA6 can trigger an apoptotic response ^[1] .

IC50 & Target

IC50: 0.6 µM (IRE1α RNase kinase) ^[2]

In Vitro

KIRA6 (1nM-100μM) bounds to the cytoplasmic domain of KIT with a K _d 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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay ^[1]

Cell Line:	HMC-1.1 cells
Concentration:	10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time:	72 hours
Result:	Inhibited cell viability from 30 nM.

Western Blot Analysis ^[1]

Cell Line:	HMC-1.1 cells
Concentration:	10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time:	1 hours
Result:	Reduced expression of phosphorylated KIT, STAT5 and ERK1/2.

RT-PCR ^[2]

Cell Line:	INS-1 IRE1α (WT) cells
Concentration:	1 μM
Incubation Time:	0 hour, 12 hours, 24 hours, 48 hours
Result:	Inhibited Ins1 mRNA expression.

Apoptosis Analysis ^[2]

Cell Line:	INS-1 IRE1α (WT) cells
Concentration:	1-10 μM
Incubation Time:	72 hours
Result:	Reduced 1NM-PP1 potentiation of Ins1 apoptosis during ER stress.

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Ins2+/Akita mice ^[2]
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; 5 mg/kg; 21 or 18 days postinjections
Result:	Attenuates b cell functional loss, increased insulin levels.

Appearance

Solid

Shipping

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

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 48.21 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9285 mL	9.6426 mL	19.2853 mL
5 mM	0.3857 mL	1.9285 mL	3.8571 mL
10 mM	0.1929 mL	0.9643 mL	1.9285 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution

* All of the co-solvents are available by MCE.