Grp94 Inhibitor-1

SKU: orb1220515

Description

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

Images & Validation

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Key Properties

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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

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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.

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.

Storage & Handling

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

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Gene Symbol

GPR

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