2. Apoptosis
  3. Bcl-2 Family
  4. GL0388

GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.

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GL0388 Chemical Structure

GL0388 Chemical Structure

CAS No. : 2886772-68-3

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Based on 1 publication(s) in Google Scholar

GL0388 Related Antibodies

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Description

GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo[1].

IC50 & Target[1]

Bax

 

In Vitro

GL0388 (0.1-10 μM; 72 h) inhibits the cell proliferation of MDA-MB-231 and MCF-7 breast cancer cell lines, with IC50s of 0.96 μM and 0.52 μM, respectively[1].
GL0388 (0.01-100 μM) inhibits the cell proliferation in 60 human tumor cell lines, with GI550s of 0.299-1.57 μM[1].
GL0388 (1-10 μM; 48 h) significantly upregulates the cleaved PARP-1 and cleaved caspase 3 in MDA-MB-231 cells[1].
GL0388 (0.1-1 μM; 24 h) inhibits the colony formation and invasion of breast cancer cells[1].
GL0388 (1-10 μM; 24 h) promotes Bax insertion into mitochondrial membranes of MDA-MB-231 cells in a dose-dependent manner. GL0388 increases cytochrome c in the cytosolic fraction of MDA-MB-231 cells[1].

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

GL0388 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MCF-7, MDA-MB-231 cells
Concentration: 0.1, 0.33, 1, 3.3, 10 μM
Incubation Time: 72 hours
Result: Inhibited the growth of MCF-7, MDA-MB-231 cells, with IC50s of 0.52 μM and 0.96 μM, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1, 5, 10 μM
Incubation Time: 48 hours
Result: Significantly led to the upregulation of cleaved PARP-1 and cleaved caspase 3.
In Vivo

GL0388 (10-20 mg/kg for i.p.; 15 mg/kg for i.t.; once daily for 10 days) dose-dependently suppresses the growth of MDA-MB-231 tumors in mice[1].

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

Animal Model: Female nude mice were injected MDA-MB-231 cells[1]
Dosage: 10-20 mg/kg for i.p.; 15 mg/kg for i.t.
Administration: I.p and i.t. once daily for 10 days
Result: Significantly inhibited tumor growth at a dose of 15 mg/kg every other day.
I.T. administration for 10 consecutive days, with an inhibition rate of 55%, comparable to the I.P. efficacy at the dose of daily 20 mg/kg.
Molecular Weight

332.37

Formula

C21H17FN2O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

NCCOC1=NC=CC=C1/C=C2C3=C(C4=C\2C=C(C=C4)F)C=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (300.87 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 3.0087 mL 15.0435 mL 30.0870 mL
5 mM 0.6017 mL 3.0087 mL 6.0174 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
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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

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Volume (start)

V1

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Concentration (final)

C2

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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: ≥ 2.5 mg/mL (7.52 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.52 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 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Dosing volume
(per animal)

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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 3.0087 mL 15.0435 mL 30.0870 mL 75.2174 mL
5 mM 0.6017 mL 3.0087 mL 6.0174 mL 15.0435 mL
10 mM 0.3009 mL 1.5043 mL 3.0087 mL 7.5217 mL
15 mM 0.2006 mL 1.0029 mL 2.0058 mL 5.0145 mL
20 mM 0.1504 mL 0.7522 mL 1.5043 mL 3.7609 mL
25 mM 0.1203 mL 0.6017 mL 1.2035 mL 3.0087 mL
30 mM 0.1003 mL 0.5014 mL 1.0029 mL 2.5072 mL
40 mM 0.0752 mL 0.3761 mL 0.7522 mL 1.8804 mL
50 mM 0.0602 mL 0.3009 mL 0.6017 mL 1.5043 mL
60 mM 0.0501 mL 0.2507 mL 0.5014 mL 1.2536 mL
80 mM 0.0376 mL 0.1880 mL 0.3761 mL 0.9402 mL
100 mM 0.0301 mL 0.1504 mL 0.3009 mL 0.7522 mL
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GL0388 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:

GL03882886772-68-3GL 0388GL-0388Bcl-2 FamilyBaxmitochondrialantiproliferativeapoptosistumorInhibitorinhibitorinhibit

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