G-5758

G-5758 is a selective and orally effective IRE1α inhibitor with an IC50 of 38 nM (detected by the XBP1s luciferase reporter cell assay) . G-5758 is still well tolerated in rats at oral doses up to 500 mg/kg. G-5758 can be used in the research of multiple myeloma[1].

Product Specifications

CAS Number

[2413455-99-7]

UNSPSC

12352005

Target

IRE1

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/g-5758.html

Concentration

10mM

Purity

98.91

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

FC1=C(F)C(NS(CC2=CC=CC=C2)(=O)=O)=C(F)C=C1OC3=C(C=CC=N3)C4=CC=NC(N[C@H]5C[C@H](F)CNC5)=N4

Molecular Formula

C27H24F4N6O3S

Molecular Weight

588.58

References & Citations

[1]Braun MG, et al. Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model. J Med Chem. 2024 Jun 13;67 (11) :8708-8729.