Grp94 Inhibitor-1

SKU: orb1220515

Description

Grp94 Inhibitor-1 is a potent selective Grp94 inhibitor (IC50 : 2 nM).

Research Area

Pharmacology & Drug Discovery; Cell Biology

Key Properties

• CAS Number: 2234897-35-7
• MW: 352.47
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₈N₂O₂
• SMILES: CC(C)c1ccc(cc1)-c1ccc(N[C@H]2CC[C@H](O)CC2)c(c1)C(N)=O
• Target: GPR
• Solubility: In Vitro: DMSO : 250 mg/mL (709.28 mM)

Bioactivity

• In Vivo:
  Grp94 Inhibitor-1 (intraperitoneal injection, qid. ; coadminbistration 10 mg/kg or 30 mg/kg; 8 days) does not attenuate the colon shortening, but decreases disease activity index (DAI) scores. It also TNFα and IL-6 levels in the serum and colonic tissues and significantly reduces the p65 expression in colonic tissues, especially those in the 30 mg/kg dose group. Animal model: C57BL/6 mice (male, 20-22 g). Dosage: 10 mg/kg or 30 mg/kg. Administration: Intraperitoneal injection, qid. ; coadminbistration 10 mg/kg or 30 mg/kg. Result: Decreased disease activity index (DAI) scores in UC mices.
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• In Vitro:
  Grp94-specific clients include a subset of integrin subunits such as integrin α2 and integrin αL. Their maturation and trafficking to the cell surface are dependent on the Grp94 chaperone function but have no association with cytoplasmic Hsp90α. Grp94 Inhibitor-1 (1-5 μM; 36 hours) significantly downregulated the cell surface expression levels of integrin α2 and integrin αL in a dose-dependent manner in panc1 cells. Western blot analysis. Cell line: Panc1 cells. Concentration: 1 μM; 2.5 μM; 5 μM Incubation time: 36 hours. Result: Decreased integrin α2 and integrin αL protein expression.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

GPR