Grp94 Inhibitor-1
Based on 5 publication(s) in Google Scholar
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.
- Purity: 98.75%
- CAS No.: 2234897-35-7
- Formula: C22H28N2O2
- Molecular Weight:352.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Grp94 Inhibitor-1
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Biological Activity
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GRP94 2 nM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Panc1 cells
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Concentration:1 μM; 2.5 μM; 5 μM
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Incubation Time:36 hours
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Result:Decreased integrin α2 and integrin αL protein expression.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (male, 20-22 g)[1]
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Dosage:10 mg/kg or 30 mg/kg
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Administration:Intraperitoneal injection,qid.; coadminbistration 10 mg/kg or 30 mg/kg
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Result:Decreased disease activity index (DAI) scores in UC mices.
Chemical Information
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CAS No. 2234897-35-7
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Appearance Solid
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Molecular Weight 352.47
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Formula C22H28N2O2
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Color Light yellow to yellow
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SMILES
O=C(C1=CC(C2=CC=C(C(C)C)C=C2)=CC=C1N[C@H]3CC[C@H](O)CC3)N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell Death Discov
The chaperone GRP94 interacts with the proprotein convertase furin and regulates TGF-beta maturation in human primary M2 macrophages. [Abstract]2025 Dec 15;11(1):558. PMID: 41397967 -
Acta Physiol
GRP94 Promotes the Fusion of Mouse C2C12 Myoblasts and the Regeneration of Skeletal Muscle Injuries Through Myomaker. [Abstract]2026 Jun;242(6):e70236. PMID: 42057593 -
Genes Immun
Comprehensive analysis of heat shock proteins in glioma revealed the association with glioma-associated myeloid cells. [Abstract]2025 Apr 15. PMID: 40234584 -
J Virol
ATF6-Mediated Unfolded Protein Response Facilitates Adeno-associated Virus 2 (AAV2) Transduction by Releasing the Suppression of the AAV Receptor on Endoplasmic Reticulum Stress. [Abstract]2022 Feb 9;96(3):e0110321. PMID: 34851146 -
Solvent & Solubility
DMSO : 175 mg/mL (496.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8371 mL | 14.1856 mL | 28.3712 mL | 70.9280 mL |
| 5 mM | 0.5674 mL | 2.8371 mL | 5.6742 mL | 14.1856 mL | |
| 10 mM | 0.2837 mL | 1.4186 mL | 2.8371 mL | 7.0928 mL | |
| 15 mM | 0.1891 mL | 0.9457 mL | 1.8914 mL | 4.7285 mL | |
| 20 mM | 0.1419 mL | 0.7093 mL | 1.4186 mL | 3.5464 mL | |
| 25 mM | 0.1135 mL | 0.5674 mL | 1.1348 mL | 2.8371 mL | |
| 30 mM | 0.0946 mL | 0.4729 mL | 0.9457 mL | 2.3643 mL | |
| 40 mM | 0.0709 mL | 0.3546 mL | 0.7093 mL | 1.7732 mL | |
| 50 mM | 0.0567 mL | 0.2837 mL | 0.5674 mL | 1.4186 mL | |
| 60 mM | 0.0473 mL | 0.2364 mL | 0.4729 mL | 1.1821 mL | |
| 80 mM | 0.0355 mL | 0.1773 mL | 0.3546 mL | 0.8866 mL | |
| 100 mM | 0.0284 mL | 0.1419 mL | 0.2837 mL | 0.7093 mL |
Grp94 Inhibitor-1 Related Classifications
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