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GRP78-IN-3

CAS No. 2707510-30-1

GRP78-IN-3( —— )

Catalog No. M36059 CAS No. 2707510-30-1

GRP78-IN-3, a potent small-molecule-competitive inhibitor of Hsp70 substrate binding and is a selective Grp78 (HSPA5) inhibitor with an IC50 of 0.59 μM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GRP78-IN-3
  • Note
    Research use only, not for human use.
  • Brief Description
    GRP78-IN-3, a potent small-molecule-competitive inhibitor of Hsp70 substrate binding and is a selective Grp78 (HSPA5) inhibitor with an IC50 of 0.59 μM.
  • Description
    GRP78-IN-3 is a selective Grp78 (HSPA5) inhibitor with an IC50 of 0.59 μM. GRP78-IN-3 is 7-fold selective for HspA5 compared to HspA9 (IC50 of 4.3 μM) and >20-fold selective for HspA5 compared to HspA2 (IC50 of 13.9 μM).
  • In Vitro
    GRP78-IN-3 (compound 8) is a potent small-molecule-competitive inhibitor of Hsp70 substrate binding. GRP78-IN-3 (0.1-100 μM) shows more potent inhibition efffects in a spheroid tumor model (U251 glioblastoma cells and H520 lung cancer cells).
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Cytoskeleton/Cell Adhesion Molecules
  • Target
    HSP
  • Recptor
    HSP
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2707510-30-1
  • Formula Weight
    342.42
  • Molecular Formula
    C17H18N4O2S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 5 mg/mL (14.60 mM; Ultrasonic )
  • SMILES
    C(N[C@H](C(NC1=NC=CS1)=O)[C@H](C)C)(=O)C2=CC=3C(N2)=CC=CC3
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Andrew J Ambrose, et al. Discovery and Development of a Selective Inhibitor of the ER Resident Chaperone Grp78. J Med Chem. 2022 Dec 14.?
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