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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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4-Br-Bnlm Chemical Structure

4-Br-Bnlm Chemical Structure

CAS No. : 1654775-71-9

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Based on 1 publication(s) in Google Scholar

4-Br-Bnlm Related Antibodies

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Description

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[1][2].

IC50 & Target

EC50: 0.96 µM (glucose-regulated protein 94, Grp94)[1][2]
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.

4-Br-Bnlm Related Antibodies

Cell Viability Assay[1]

Cell Line: Primary human HTM cells.
Concentration: 30 µM.
Incubation Time: 24 h.
Result: Significantly reduced the level of Y437H mutant myocilin without affecting WT myocilin and the RFP vector in HEK cells.

Western Blot Analysis[1]

Cell Line: HEK cells.
Concentration: 0, 1, 3, 10, 30 and 100 µM.
Incubation Time: 24 h.
Result: Significantly decreased 1477N mutant myocilin in HEK cells expression without causing the degradation of other Hsp90-dependent clients Akt and Ras.
In Vivo

4-Br-Bnlm (300 µM; eye drops; once daily for 12 weeks) clears the mutant myocilin within trabecular meshwork (TM) cells and decreases intraocular pressure (IOP) in Tg-MYOCY437H mice model. 4-Br-Bnlm improves photopic negative response (PhNR) deficits[2].

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

Animal Model: Tg-MYOCY437H mice[2].
Dosage: 300 µM.
Administration: Eye drops; once daily for 12 weeks.
Result: Inhibited mutant myocilin expression and restored the PhNR deficits.
Molecular Weight

465.72

Formula

C20H18BrClN2O4
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(OC)C1=C(O)C=C(O)C(Cl)=C1CCC2=NC=CN2CC3=CC=C(Br)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1472 mL 10.7361 mL 21.4721 mL
5 mM 0.4294 mL 2.1472 mL 4.2944 mL
View the 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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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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% 
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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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, 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
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
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4-Br-Bnlm Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

4-Br-Bnlm1654775-71-9OthersHEKHTMiHEK WTMiceMyocilinInhibitorinhibitorinhibit

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