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

GL0388 

Cat. No.: HY-132173 Purity: 98.01%
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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.

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

GL0388 Chemical Structure

GL0388 Chemical Structure

CAS No. : 2886772-68-3

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5 mg USD 265 In-stock
10 mg USD 420 In-stock
25 mg USD 860 In-stock
50 mg USD 1420 In-stock
100 mg USD 2200 In-stock
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Based on 1 publication(s) in Google Scholar

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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.

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)

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
10 mM 0.3009 mL 1.5043 mL 3.0087 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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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.

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Product Name:
GL0388
Cat. No.:
HY-132173
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