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PBOX 6

Catalog No. T16436 CAS 290814-68-5

Synonyms: PBOX-6

PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX) compound with anticancer and antitumor activity that inhibits breast cancer cell growth in vitro and selectively induces apoptosis in leukemia cells via c-Jun NH2 terminal kinase-dependent phosphorylation and inactivation of Bcl-2 and Bcl-XL.

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PBOX 6, CAS 290814-68-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
2 mg	In stock	$ 76.00
5 mg	In stock	$ 134.00
1 mL * 10 mM (in DMSO)	In stock	$ 143.00

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Purity: 98.18%

Biological Description

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Description

In vitro

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

Synonyms	PBOX-6
Molecular Weight	396.44
Formula	C25H20N2O3
CAS No.	290814-68-5

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (75.67 mM), Sonication is recommended.

References and Literature

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. 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. 3. 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.

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Keywords

PBOX 6 290814-68-5 Apoptosis PBOX-6 PBOX6 inhibitor inhibit

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