1. Cell Cycle/DNA Damage
  2. IRE1
  3. KIRA6

KIRA6 

Cat. No.: HY-19708 Purity: 99.86%
Handling Instructions

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

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

KIRA6 Chemical Structure

KIRA6 Chemical Structure

CAS No. : 1589527-65-0

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 125 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 125 In-stock
Estimated Time of Arrival: December 31
Solid
1 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 170 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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Description

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].

IC50 & Target

IC50: 0.6 µM (IRE1α RNase kinase)[2]

In Vitro

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].

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.
Molecular Weight

518.53

Formula

C₂₈H₂₅F₃N₆O

CAS No.
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 : 6.25 mg/mL (12.05 mM; Need ultrasonic)

Ethanol : 2 mg/mL (3.86 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 provided by MCE.
References

Purity: 99.86%

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KIRA6
Cat. No.:
HY-19708
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