2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. GRP78-IN-3

GRP78-IN-3 (Compound 8) is a selective Grp78 (HSPA5) inhibitor with an IC50 of 0.59 μM. GRP78-IN-3 is 7-fold selective for HspA5 compared to HspA9 (IC50 of 4.3 μM) and >20-fold selective for HspA5 compared to HspA2 (IC50 of 13.9 μM).

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

GRP78-IN-3 Chemical Structure

GRP78-IN-3 Chemical Structure

CAS No. : 2707510-30-1

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Based on 1 publication(s) in Google Scholar

GRP78-IN-3 Related Antibodies

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View All HSP Isoform Specific Products:

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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Description

GRP78-IN-3 (Compound 8) is a selective Grp78 (HSPA5) inhibitor with an IC50 of 0.59 μM. GRP78-IN-3 is 7-fold selective for HspA5 compared to HspA9 (IC50 of 4.3 μM) and >20-fold selective for HspA5 compared to HspA2 (IC50 of 13.9 μM)[1].

IC50 & Target[1]

HSPA5

0.59 μM (IC50)

In Vitro

GRP78-IN-3 (compound 8) is a potent small-molecule-competitive inhibitor of Hsp70 substrate binding. GRP78-IN-3 (0.1-100 μM) shows more potent inhibition efffects in a spheroid tumor model (U251 glioblastoma cells and H520 lung cancer cells)[1].

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

GRP78-IN-3 Related Antibodies
Molecular Weight

342.42

Formula

C17H18N4O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC2=C(N1)C=CC=C2)N[C@H](C(NC3=NC=CS3)=O)C(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (14.60 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 2.9204 mL 14.6020 mL 29.2039 mL
5 mM 0.5841 mL 2.9204 mL 5.8408 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 0.5 mg/mL (1.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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: ≥ 0.5 mg/mL (1.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 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 (5.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).
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. 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 2.9204 mL 14.6020 mL 29.2039 mL 73.0098 mL
5 mM 0.5841 mL 2.9204 mL 5.8408 mL 14.6020 mL
10 mM 0.2920 mL 1.4602 mL 2.9204 mL 7.3010 mL
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GRP78-IN-3 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:

GRP78-IN-32707510-30-1HSPHeat shock proteinsGrp78HSPA5endoplasmic reticulum (ER) stressInhibitorinhibitorinhibit

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