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KIRA6

Catalog No. TQ0076 CAS 1589527-65-0

KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.

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KIRA6, CAS 1589527-65-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 91.00
10 mg	In stock	$ 140.00
25 mg	In stock	$ 286.00
50 mg	In stock	$ 413.00
100 mg	In stock	$ 615.00
1 mL * 10 mM (in DMSO)	In stock	$ 109.00

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Purity: 100%

Biological Description

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Description	KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.
Targets&IC50	IRE1α:0.6 µM (cell free)
In vitro	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. KIRA6 (1nM-100μM) bounds to the cytoplasmic domain of KIT with a Kd value of 10.8 ?μM. 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 in a dose-dependent manner. KIRA6 (0.1-10μM, 72 hours) dose-dependently reduces 1NM-PP1 potentiation of Ins1 apoptosis during ER stress in a dose-dependent manner [2].
In vivo	KIRA6 (intraperitoneal injection; 5 mg/kg; 37 days) shows significant amelioration of random glucose levels over several weeks compared to the vehicle, both fed ad lib. KIRA6 (i.p, 5 mg/kg, 21 or 18 days post injections) increases both plasma insulin and C-peptide levels, remains insulin-positive islet areas at a high level after stopping injections in the Akita Mouse [2].
Cell Research	Cell Line: HMC-1.1 cells. Concentration: 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM. Incubation Time: 72 hours [1]
Animal Research	Animal Model: Male Ins2+/Akita mice. Dosage: 5 mg/kg. Administration: Intraperitoneal injection, 5 mg/kg, 21 or 18 days post injections [2]

Molecular Weight	518.53
Formula	C28H25F3N6O
CAS No.	1589527-65-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 2 mg/mL (3.86 mM), Sonification is recommended.

DMSO: 5 mg/mL (9.64 mM)

References and Literature

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.

Citations

1. Wang J, Zhang J, Guo Z, et al.Targeting HSP70 chaperones by rhein sensitizes liver cancer to artemisinin derivatives.Phytomedicine.2023: 155156.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Covalent Inhibitor Library NO PAINS Compound Library Endoplasmic Reticulum Stress Compound Library Bioactive Compound Library Anti-Diabetic Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library Immunology/Inflammation Compound Library Cell Cycle Compound Library

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MKC8866 GSK2850163 IRE1α kinase-IN-8 IRE1α kinase-IN-9 4μ8C Toyocamycin STF-083010 APY29

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Keywords

KIRA6 1589527-65-0 Cell Cycle/Checkpoint IRE1 Inhibitor KIRA 6 Inositol requiring enzyme 1 inhibit KIRA-6 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.