Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
    English |     Chinese

Product Inquiry: sales@probechem.com
Order/PO receiving: order@probechem.com

You are here:Home-Chemical Inhibitors & Agonists-Nuclear Receptor/Transcription Factor-IRE1-G-5758
G-5758

Chemical Structure : G-5758

CAS No.: 2413455-99-7

Add to Favorites

G-5758 (G5758)

Catalog No.: PC-22293Not For Human Use, Lab Use Only.

G-5758 (G5758) is a potent and selective, orally active IRE1α inhibitor with IC50 of 0.27 nM in HTRF IRE1α binding assays, inhibits IRE1α-Rnase with IC50 of 4.3 nM.

Packing Price Stock Quantity
50 mg Get quote
100 mg Get quote
250 mg Get quote
Get Quotation Now
* Please select Quantity before adding items.
 or Bulk Inquiry

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Purity & Documentation Purity: >98% (HPLC)

Biological Activity

G-5758 (G5758) is a potent and selective, orally active IRE1α inhibitor with IC50 of 0.27 nM in HTRF IRE1α binding assays, inhibits IRE1α-Rnase with IC50 of 4.3 nM.
G-5758 potently inhibits XBP1 splicing with IC50 of 38 nM in cellular XBP1s luciferase reporter assay.
G-5758 displays 100-fold more selective against 219 kinases and at least 83-fold selective against HIPK4.
G-5758 demonstrated a robust PD response to induced IRE1 knockdown in the sh9/8 KMS-11 xenograft model.

Physicochemical Properties

M.Wt 588.58
Formula C27H24F4N6O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-Phenyl-N-(2,3,6-trifluoro-4-((3-(2-(((3S,5S)-5-fluoropiperidin-3-yl)amino)pyrimidin-4-yl)pyridin-2-yl)oxy)phenyl)methanesulfonamide

References

1. Braun MG, et al. J Med Chem. 2024 May 15. doi: 10.1021/acs.jmedchem.3c02425.

Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

Contact Us sales@probechem.com

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • *Additional Information:

Get Quote

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • Additional Information: