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PK-11195 | Mitochondrial benzodiazepine receptor ligand

PK-11195 (85532-75-8) is a selective and potent peripheral benzodiazepine receptor, PBR (or TSPO, translocator protein) antagonist.1,2 It has been shown to chemosensitize tumor cells to a variety of chemotherapeutic agents via PBR-independent pathways.3,4 PK-11195 is also able to induce apoptosis in a variety of cell lines.5-7

References/Citations
1) Le Fur, et al.; (1983) Peripheral benzodiazepine binding sites: effect of PK 11195, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide. I. In vitro studies; Life Sci., 32 1839
2) Le Fur et al.; (1983) Peripheral benzodiazepine binding sites: effect of PK 11195, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide. II. In vivo studies; Life Sci., 32 1849
3) Gonzalez-Polo et al. (2005) PK11195 potently sensitizes to apoptosis induction independently from the peripheral benzodiazepine receptor; Oncogene, 24 7503
4) Walter et al. (2005) PK11195, a peripheral benzodiazepine receptor (pBR) ligand, broadly blocks drug efflux to chemosensitize leukemia and myeloma cells by a pBR-independent, direct transporter-modulating mechanism; Blood, 106 3584
5) Chelli et al. (2004) Peripheral benzodiazepine receptor ligands:mitochondrial transmembrane potential depolarization and apoptosis induction in rat C6 glioma cells; Biochem. Pharmacol., 68 125
6) Sutter et al. (2004) Peripheral benzodiazepine receptor ligands induce apoptosis and cell cycle arrest in human hepatocellular carcinoma cells and enhance chemosensitivity to paclitaxel, docetaxel, doxorubicin and the Bcl-2-inhibitor HA14-1; J. Hepatol., 120 1212
7) Maaser et al. (2001) Specific ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in human colorectal cancer cells; Br. J. Cancer, 85 1771

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Focus Biomolecules supplier, chemical structure of PK-11195 | Mitochondrial benzodiazepine receptor ligand | CAS 85532-75-8

Catalog#  10-2221

$35.00
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CAS:
85532-75-8
Catalog Number:
10-2221
Activity:
Mitochondrial benzodiazepine receptor ligand
Chemical Name:
1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
Molecular Weight:
352.86
Molecular Formula:
C21H21ClN2O
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 15 mg/ml).
Physical Properties:
White solid
Storage Temperature:
RT
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored under nitrogen or argon at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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