1. Apoptosis
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  3. GL0388

GL0388 

Cat. No.: HY-132173
Handling Instructions

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

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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].

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].

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

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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

GL0388GL 0388GL-0388Bcl-2 FamilyBaxmitochondrialantiproliferativeapoptosistumorInhibitorinhibitorinhibit

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GL0388
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HY-132173
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