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[CAS NO. 1589527-65-0] KIRA6
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-19708 |
| Brand: | MCE |
| CAS: | 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 |
10 Publications Citing Use of MCE
- [1]Science. 2019 Jul 19;365(6450):eaau6499.
- [2]Nano Today. April 2022, 101416.
- [3]ACS Nano. 2021 Aug 20.
- [4]ACS Cent Sci. 2020 Jan 22;6(1):76-82.
- [5]Biomaterials. 2021, 120757.
- [6]J Control Release. 2022 Jul 5;S0168-3659(22)00401-1.
- [7]Int J Mol Sci. 2021, 22(6), 3063.
- [8]J Biol Chem. 2022 Apr 29;101997.
- [9]Mol Biol Rep. 2022 Jul 20.
- [10]Fish Shellfish Immunol. 2020 Mar;98:112-121.
Summary
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
DMSO : 25 mg/mL ( 48.21 mM ; Need ultrasonic)
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 |
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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