[CAS NO. 2121989-91-9] GSK2850163
PRODUCTS SPECIFICATIONS [2121989-91-9]
DESCRIPTION [2121989-91-9]
Overview
| MDL | MFCD30491882 |
|---|---|
| Molecular Weight | 446.41 |
| Molecular Formula | C24H29Cl2N3O |
| SMILES | O=C(N(CCC1)C[C@]21CCN(CC3=CC=C(Cl)C(Cl)=C3)C2)NCC4=CC=C(C)C=C4 |
2 Publications Citing Use of MCE
Summary
GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha ( IRE1α ) which can inhibit IRE1α kinase activity and RNase activity with IC 50 s of 20 and 200 nM, respectively.
IC50 & Target
IC50: 20 nM (IRE1α kinase activity), 200 nM (IRE1α RNase activity) [1]
In Vitro
GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC 50 s of 20 and 200 nM, respectively. The increased autophosphorylation of IRE1α could be reduced in a dose-dependent manner by GSK2850163. Increasing concentrations of GSK2850163 are capable of reducing the increased XBP 1 transcriptional activity. Two additional kinases are weakly inhibited by GSK2850163: Ron (IC 50 =4.4 μM) and FGFR1 V561M (IC 50 =17 μM) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Oil
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Pure form | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 67.5 mg/mL ( 151.21 mM ; Need ultrasonic)
Ethanol : 50 mg/mL ( 112.00 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2401 mL | 11.2005 mL | 22.4009 mL |
| 5 mM | 0.4480 mL | 2.2401 mL | 4.4802 mL |
| 10 mM | 0.2240 mL | 1.1200 mL | 2.2401 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.25 mg/mL (5.04 mM); Clear solution