NPC-15437
NPC-15437 is a selective PKC inhibitor with an IC50 of 19 µM. NPC-15437 competitively inhibits phorbol ester- (Ki of 5 µM) and phosphatidylserine-induced (Ki of 12 µM) PKC activity. NPC-15437 does not inhibits cAMP-dependent or calcium/calmodulin-dependent protein kinases. NPC-15437 augments TRAIL-induced cell death in non-small cell lung cancer and medulloblastoma cells. NPC-15437 can be used for the research of non-small cell lung cancer, medulloblastoma, and neurological disease.
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- CAS No.: 136449-85-9
- 화학식: C25H50N4O2
- 분자량:438.70
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
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PKC 19 μM (IC50) |
In Vitro
NPC-15437 (4-10 μM; 24-48 h) augments TRAIL-induced cell death and mitochondrial membrane potential loss in A549 and DAOY cells (up to 69% and 76% cell death, respectively, at 48 hours) but does not sensitize to TNFα; effect is caspase-dependent in A549 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NPC-15437 (0.01-10 mg/kg; i.p.; once) induces selective dose-dependent deficits in retention of the temporal component of a Y-maze active avoidance task in male Swiss mice (2 months old, 30-40 g) model of memory impairment[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (male, 225-250 g) bearing reward-related learning[1]
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Dosage:0.1, 0.5, 1.0 μg/0.5 μL/side
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Administration:intra-NAc; during conditioning sessions on days 1, 3, 5, 7
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Result:Dose-dependently blocked amphetamine-induced conditioned place preference: the 0.1 μg dose did not block the preference (significant increase in drug-paired compartment time from pre-conditioning to test), the 0.5 μg dose partially blocked it (no significant increase in drug-paired compartment time), and the 1.0 μg dose fully blocked it (no significant increase in drug-paired compartment time).
Did not produce a place preference or aversion when administered alone (1.0 μg, no significant change in drug-paired compartment time from pre-conditioning to test).
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Animal Model:Swiss mice (male, 2 months old, 30-40 g)[2]
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Dosage:0.01, 0.1, 1, 10 mg/kg (post-training); 1 mg/kg (pre-training and pre-retention for some groups)
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Administration:i.p.; single injection (immediately post-training, 30 minutes pre-training, 48 hours later pre-retention for some groups)
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Result:Significantly impaired retention of the temporal component with more avoidance errors versus controls at 0.1, 1, 10 mg/kg post-training; Made more avoidance errors than discrimination errors at 1 and 10 mg/kg post-training; Did not affect acquisition performance with 1 mg/kg pre-training; Impaired temporal component retention when 1 mg/kg given before acquisition regardless of pre-retention injection.
Chemical Information
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CAS No. 136449-85-9
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분자량 438.70
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화학식 C25H50N4O2
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SMILES
C(NC([C@H](CCCCN)N)=O)C1N(C(CCCCCCCCCCCC)=O)CCCC1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Aujla H, et al. Intra-accumbens protein kinase C inhibitor NPC 15437 blocks amphetamine-produced conditioned place preference in rats. Behav Brain Res. 2003;147(1-2):41-48. [Content Brief]
[2]. Mathis C, et al. The selective protein kinase C inhibitor, NPC 15437, induces specific deficits in memory retention in mice. Eur J Pharmacol. 1992;220(1):107-110. [Content Brief]
[3]. Felber M, et al. Inhibition of novel protein kinase C-epsilon augments TRAIL-induced cell death in A549 lung cancer cells. Pathol Oncol Res. 2007;13(4):295-301. [Content Brief]
[4]. Sullivan JP, et al. 2,6-Diamino-N-([1-(1-oxotridecyl)-2-piperidinyl] methyl)hexanamide (NPC 15437): a novel inhibitor of protein kinase C interacting at the regulatory domain. Mol Pharmacol. 1992 Jan;41(1):38-44. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NPC-15437 Related Classifications
HY-129980A Related Classifications
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