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PK 11195 (1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide)

Cat no: 045157

PK 11195 (1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide)

Selective peripheral benzodiazepine antagonist. Apoptosis enhancer. Glucose-induced insulin secretion inhibitor. Induces mitochondria cytochrome c release. Anticancer compound. Antiproliferative. Pharmacological tool in autophagy.\n\nStorage and Stability:\nShort-term Storage: +4 degrees C\nLong-term Storage: +4 degrees C\nStable for at least 2 years after receipt when stored at +4 degrees C.

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SPECIFICATIONS

Catalog Number

045157

Size

10mg

Purity

>98% (NMR)

References

Product Reference: \n?Differentiation between two ligands for peripheral benzodiazepine binding sites,RO5-4864 andPK 11195, by thermodynamic studies: G. Le Fur et al.; Life Sci. 33, 449 (1983) \n?Dihydropyridine and peripheral type benzodiazepine binding sites: subcellular distribution and molecular size determination: A. Doble et al.; Eur. J. Pharmacol. 119, 153 (1985) \n?PK11195, a ligand of the mitochondrial benzodiazepine receptor, facilitates the induction of apoptosis and reverses Bcl-2-mediated cytoprotection: T. Hirsch et al.; Exp. Cell. Res. 241, 426 (1998) \n?Inhibition of glucose-induced insulin secretion by a peripheral-type benzodiazepine receptor ligand (PK11195): D. Pujalte, et al.; Naunyn Schmiedebergs Arch. Pharmacol. 362, 46 (2000)\n?PK11195 potently sensitizes to apoptosis induction independently from the peripheral benzodiazepin receptor: R.A. Gonzalez-Polo, et al.; Oncogene 24, 7503 (2005) \n?Peripheral benzodiazepine receptor ligand, PK11195 induces mitochondria cytochrome c release and dissipation of mitochondria potential via induction of mitochondria permeability transition: J. Li, et al.; Eur. J. Pharmacol. 560, 117 (2007) \n?The potential anticancer agent PK11195 induces apoptosis irrespective of p53 and ATM status in chronic lymphocytic leukemia cells: A.F. Santidrian et al.; Haematologica 92, 1631 (2007) \n?Modulation of intracellular Ca2+ signalling in HeLa cells by the apoptotic cell death enhancer PK11195: M. Campanella et al.; Biochem. Pharmacol. 76, 1628 (2008) \n?Antiproliferative effect of peripheral benzodiazepine receptor antagonist PK11195 in rat mammary tumor cells: S. Mukhopadhyay et al.; Mol. Cell. Biochem. 340, 203 (2010) \n?Ca2+-dependent autophagy is enhanced by the pharmacological agent PK11195: Pharmacological tools in autophagy: A. Gastaldello, et al.; Autophagy 6 607 (2010) \n?

Alternative Names

1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide

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