1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP
  3. Grp94 Inhibitor-1

Grp94 Inhibitor-1 

Cat. No.: HY-112910 Purity: 99.18%
Handling Instructions

Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.

For research use only. We do not sell to patients.

Grp94 Inhibitor-1 Chemical Structure

Grp94 Inhibitor-1 Chemical Structure

CAS No. : 2234897-35-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 80 In-stock
Estimated Time of Arrival: December 31
50 mg USD 240 In-stock
Estimated Time of Arrival: December 31
100 mg USD 410 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α[1].

IC50 & Target[1]

GRP94

2 nM (IC50)

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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.
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (male, 20-22 g)[1]
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.
Molecular Weight

352.47

Formula

C₂₂H₂₈N₂O₂

CAS No.

2234897-35-7

SMILES

O=C(C1=CC(C2=CC=C(C(C)C)C=C2)=CC=C1N[[email protected]]3CC[[email protected]](O)CC3)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (709.28 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8371 mL 14.1856 mL 28.3712 mL
5 mM 0.5674 mL 2.8371 mL 5.6742 mL
10 mM 0.2837 mL 1.4186 mL 2.8371 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Grp94 Inhibitor-1HSPHeat shock proteinsGrp94UC integrin α2integrin αLInhibitorinhibitorinhibit

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Product Name:
Grp94 Inhibitor-1
Cat. No.:
HY-112910
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