KIRA6 free base · Synonyms: KIRA-6 · KIRA 6

KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor.

For research use only. Not for human or veterinary use.

Target IRE1

Research area Metabolic Disease Inflammation/Immunology Cancer

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Data Sheet SDS COA

KIRA6 structure

CAS No.: 1589527-65-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 385.00	BP-02139-100mg	In stock	Get quote
250 mg	USD 662.00	BP-02139-250mg	In stock	Get quote
500 mg	USD 885.00	BP-02139-500mg	In stock	Get quote
1 g	USD 1,392.00	BP-02139-1g	In stock	Get quote
5 g	USD 3,967.00	BP-02139-5g	In stock	Get quote
10 g	USD 5,893.00	BP-02139-10g	In stock	Get quote

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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.

Biological activity

In Vitro KIRA6 (1nM-100μM) bounds to the cytoplasmic domain of KIT with a Kd value of 10.8 ?μM. 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 (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. KIRA6 (1 μM; 0-48 hours) inhibits Ins1 mRNA decay from IRE1α hyperactivation at 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. 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. 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.

Identifiers

SMILES: CC(C)(C)C1=NC(=C2N1C=CN=C2N)C1=C2C=CC=CC2=C(NC(=O)NC2=CC=CC(=C2)C(F)(F)F)C=C1
InChIKey: NOHQEAFAESMMDX-UHFFFAOYSA-N

Specifications

MW (average): 518.5329
Formula: C₂₈H₂₅F₃N₆O
CAS No.: 1589527-65-0
Physical state: Solid
Color: off-white to gray
Shipping: 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: Powder 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 25 mg/mL

Documents

References

[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.

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