4-Br-Bnlm
Based on 1 Customer Validation
4-Br-Bnlm is a selective inhibitor of glucose-regulated protein 94 (Grp94) with an EC50 value of 0.96 µM. 4-Br-Bnlm reduces the levels of mutant myocilin proteins as well as wild-type myocilin misfold in cells. 4-Br-Bnlm promotes the clearance of toxic formsof myocilin and reduces myocilin toxicity.
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- Pureté : 99.46%
- CAS No.: 1654775-71-9
- Formule: C20H18BrClN2O4
- Masse moléculaire:465.72
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
In Vitro
4-Br-Bnlm (0-100 µM; 24 h) inhibits 1477N mutant myocilin in human embryonic kidney (HEK) cells expression[1].
4-Br-Bnlm (30 µM; 24 h) reduces mutant myocilin levels and toxicity in primary human trabecular meshwork (HTM) cells[1].
4-Br-Bnlm (3, 10 and 30 µM; 24 h) inhibits myocilin secretion with dose-dependent manner in myocilin cell[1].
4-Br-Bnlm (30 µM and 100 µM; 24 h) doesn’t induces a heat shock response in the HTM cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary human HTM cells.
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Concentration:30 µM.
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Incubation Time:24 h.
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Result:Significantly reduced the level of Y437H mutant myocilin without affecting WT myocilin and the RFP vector in HEK cells.
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Cell Line:HEK cells.
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Concentration:0, 1, 3, 10, 30 and 100 µM.
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Incubation Time:24 h.
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Result:Significantly decreased 1477N mutant myocilin in HEK cells expression without causing the degradation of other Hsp90-dependent clients Akt and Ras.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Tg-MYOCY437H mice[2].
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Dosage:300 µM.
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Administration:Eye drops; once daily for 12 weeks.
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Result:Inhibited mutant myocilin expression and restored the PhNR deficits.
Chemical Information
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CAS No. 1654775-71-9
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Appearance Solid
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Masse moléculaire 465.72
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Formule C20H18BrClN2O4
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Color Off-white to light yellow
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SMILES
O=C(OC)C1=C(O)C=C(O)C(Cl)=C1CCC2=NC=CN2CC3=CC=C(Br)C=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
In Vitro:
DMSO : 33.33 mg/mL (71.57 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.5 mg/mL (5.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Stothert AR, et al, Fontaine SN, Crowley VM, Mishra S, Blagg BS, Lieberman RL, Dickey CA. Exploiting the interaction between Grp94 and aggregated myocilin to treat glaucoma. Hum Mol Genet. 2014 Dec 15;23(24):6470-80. [Content Brief]
[2]. Stothert AR, et al. Isoform-selective Hsp90 inhibition rescues model of hereditary open-angle glaucoma. Sci Rep. 2017 Dec 20;7(1):17951. [Content Brief]
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1472 mL | 10.7361 mL | 21.4721 mL | 53.6803 mL |
| 5 mM | 0.4294 mL | 2.1472 mL | 4.2944 mL | 10.7361 mL | |
| 10 mM | 0.2147 mL | 1.0736 mL | 2.1472 mL | 5.3680 mL | |
| 15 mM | 0.1431 mL | 0.7157 mL | 1.4315 mL | 3.5787 mL | |
| 20 mM | 0.1074 mL | 0.5368 mL | 1.0736 mL | 2.6840 mL | |
| 25 mM | 0.0859 mL | 0.4294 mL | 0.8589 mL | 2.1472 mL | |
| 30 mM | 0.0716 mL | 0.3579 mL | 0.7157 mL | 1.7893 mL | |
| 40 mM | 0.0537 mL | 0.2684 mL | 0.5368 mL | 1.3420 mL | |
| 50 mM | 0.0429 mL | 0.2147 mL | 0.4294 mL | 1.0736 mL | |
| 60 mM | 0.0358 mL | 0.1789 mL | 0.3579 mL | 0.8947 mL |
4-Br-Bnlm Related Classifications
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