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PBOX 6

Catalog No.GC33002

PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX) compound, acts as a microtubule-depolymerizing agent and an apoptotic agent.

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PBOX 6 Chemical Structure

Cas No.: 290814-68-5

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5mg
$144.00
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10mg
$185.00
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25mg
$387.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

Cells are seeded at a density of 3 × 105 cells/mL and following treatment with the indicated compound (including PBOX 6), an aliquot (100 μL) is cytocentrifuged onto glass slides precoated with poly(l-lysine). They are then stained with the RapiDiff kit (eosin/methylene blue). The degree of apoptosis and necrosis is determined by counting 300 cells under a light microscope. At least three fields of view per slide, with an average of 100 cells per field, are counted and the percentage of apoptosis and necrosis is determined. Apoptotic cells are characterized by cell shrinkage, membrane blebbing, and nuclear condensation and fragmentation, whereas necrotic cells are identified by cell swelling and loss of cell membrane[1].

References:

[1]. Zisterer DM, et al. Pyrrolo-1,5-benzoxazepines induce apoptosis in HL-60, Jurkat, and Hut-78 cells: a new class of apoptotic agents. J Pharmacol Exp Ther. 2000 Apr;293(1):48-59.
[2]. Mc Gee MM, et al. Caspase-3 is not essential for DNA fragmentation in MCF-7 cells during apoptosis induced by the pyrrolo-1,5-benzoxazepine, PBOX-6. FEBS Lett. 2002 Mar 27;515(1-3):66-70.
[3]. Bane FT, et al. The microtubule-targeting agents, PBOX-6 [pyrrolobenzoxazepine 7-[(dimethylcarbamoyl)oxy]-6-(2-naphthyl)pyrrolo-[2,1-d] (1,5)-benzoxazepine] and paclitaxel, induce nucleocytoplasmic redistribution of the peptidyl-prolyl isomerases, cyclophilin A and pin1, in malignant hematopoietic cells. J Pharmacol Exp Ther. 2009 Apr;329(1):38-47.

Background

PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX) compound, acts as a microtubule-depolymerizing agent and an apoptotic agent.

PBOX 6 is a potent apoptotic PBOX, but does not elicit a general toxic effect in a rat R2C Leydig cell line. PBOX 6 (0-25 μM, 16 h) results in dose- and time-dependent induction of apoptosis, and also causes DNA fragmentation at 10 μM in HL-60 cells. PBOX 6 (10 μM) induces apoptosis through activation of caspase 3-like proteases in HL-60 cells. PBOX 6 (10 μM) induces apoptosis and exerts an accumulation of cytochromec in the cytosol, but this effect is not triggered by oxidative stress, and is independent of peripheral-type benzodiazepine receptor (PBR) and NF-κB[1]. PBOX 6 (25 μM) induces apoptosis in MCF-7 cells through activation of caspase-7[2]. PBOX 6 (10 μM) induces the redistribution of cypA from the nucleus to the cytosol of the cell in K562 cells. PBOX 6 (10 μM) induces nucleocytoplasmic redistribution of cypA and pin1 through a JNK-dependent manner, also dependent on upstream activation of a trypsin-like serine protease, and this effect correlates with G2/M arrest in K562 cells[3].

[1]. Zisterer DM, et al. Pyrrolo-1,5-benzoxazepines induce apoptosis in HL-60, Jurkat, and Hut-78 cells: a new class of apoptotic agents. J Pharmacol Exp Ther. 2000 Apr;293(1):48-59. [2]. Mc Gee MM, et al. Caspase-3 is not essential for DNA fragmentation in MCF-7 cells during apoptosis induced by the pyrrolo-1,5-benzoxazepine, PBOX-6. FEBS Lett. 2002 Mar 27;515(1-3):66-70. [3]. Bane FT, et al. The microtubule-targeting agents, PBOX-6 [pyrrolobenzoxazepine 7-[(dimethylcarbamoyl)oxy]-6-(2-naphthyl)pyrrolo-[2,1-d] (1,5)-benzoxazepine] and paclitaxel, induce nucleocytoplasmic redistribution of the peptidyl-prolyl isomerases, cyclophilin A and pin1, in malignant hematopoietic cells. J Pharmacol Exp Ther. 2009 Apr;329(1):38-47.

Chemical Properties

Cas No. 290814-68-5 SDF
Canonical SMILES O=C(OC1=C(C2=C3C=CC=CC3=CC=C2)OC4=CC=CC=C4N5C1=CC=C5)N(C)C
Formula C25H20N2O3 M.Wt 396.44
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.5224 mL 12.6122 mL 25.2245 mL
5 mM 0.5045 mL 2.5224 mL 5.0449 mL
10 mM 0.2522 mL 1.2612 mL 2.5224 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 26 reference(s) in Google Scholar.)

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