2. 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.

For research use only. We do not sell to patients.

NPC-15437

NPC-15437 Chemical Structure

CAS No. : 136449-85-9

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Description

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[1][2][3][4].

IC50 & Target

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.

NPC-15437 Related Antibodies
In Vivo

NPC-15437 (0.1-1.0 μg/0.5 μL/side; intra-NAc; during conditioning sessions on days 1, 3, 5, 7) blocks drug-induced conditioned place preference in male Wistar rats (225-250 g) with reward-related learning[1].
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.

Animal Model: Wistar rats (male, 225-250 g) bearing reward-related learning[1]
Dosage: 0.1, 0.5, 1.0 μg/0.5 μL/side
Administration: intra-NAc; during conditioning sessions on days 1, 3, 5, 7
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).
Animal Model: Swiss mice (male, 2 months old, 30-40 g)[2]
Dosage: 0.01, 0.1, 1, 10 mg/kg (post-training); 1 mg/kg (pre-training and pre-retention for some groups)
Administration: i.p.; single injection (immediately post-training, 30 minutes pre-training, 48 hours later pre-retention for some groups)
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.
Molecular Weight

438.70

Formula

C25H50N4O2
CAS No.
SMILES

C(NC([C@H](CCCCN)N)=O)C1N(C(CCCCCCCCCCCC)=O)CCCC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NPC-15437 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NPC-15437136449-85-9NPC15437NPC 15437conventional PKCcPKCTRAILDAOYneurological diseasenovel PKCA549non-small cell lung cancerPKCεnPKCmale Wistar ratsTNFαY-maze active avoidance taskmicePKCratsmedulloblastomamale Swiss miceprotein kinase CInhibitorinhibitorinhibit

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