Grp94 Inhibitor-1 [2234897-35-7]
Référence T7261-10mg
Conditionnement : 10mg
Marque : TargetMol
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Grp94 Inhibitor-1
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Grp94 Inhibitor-1 is a potent and selective inhibitor of Grp94 with an IC50 of 2 nM.
Cas No. 2234897-35-7
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:98.83%
Appearance:Solid
Color:White
COA LCMS HNMR
Product Introduction
Grp94 Inhibitor-1 AI Summary
Grp94 Inhibitor-1 exhibits potent bioactivity related to its binding affinity and inhibition properties on chaperone proteins HSP90alpha and GRP94. It demonstrates high binding affinity to both human HSP90alpha and dog GRP94 proteins, with Kd values around 20,000 nM. The compound shows strong inhibition of FITC-geldanamycin binding to the dog GST-tagged GRP94 protein, achieving an IC50 value of 2.0 nM and complete inhibition at a concentration of 100 uM. Additionally, the compound achieves 100% inhibition of both dog GRP94 and HSP90alpha at the same concentration. Grp94 Inhibitor-1 has favorable pharmacokinetic properties, including a logD value of 4.59, adequate aqueous solubility at 3.9 ug/mL, high permeability at pH 7.4, and stable metabolic characteristics in both mouse and human microsomes. These activities suggest that Grp94 Inhibitor-1 may have potential as a modulator of HSP90alpha and GRP94 protein interactions..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Grp94 Inhibitor-1 is a potent and selective inhibitor of Grp94 with an IC50 of 2 nM. |
| Targets & IC50 | Grp94:2 nM |
| Molecular Weight | 352.47 |
| Formula | C22H28N2O2 |
| Cas No. | 2234897-35-7 |
| Smiles | CC(C)c1ccc(cc1)-c1ccc(N[C@H]2CC[C@H](O)CC2)c(c1)C(N)=O |
| Relative Density. | 1.165 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 83.33 mg/mL (236.42 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.67 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||