NPC-15437 hydrochloride | CAS# 141774-20-1 | PKC inhibitor

MedKoo Cat#: 574806 | Name: NPC-15437 hydrochloride

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

NPC-15437 hydrochloride is a selective protein kinase C (PKC) inhibitor.

Chemical Structure

NPC-15437 hydrochloride

CAS#141774-20-1

Theoretical Analysis

MedKoo Cat#: 574806

Name: NPC-15437 hydrochloride

CAS#: 141774-20-1

Chemical Formula: C25H52Cl2N4O2

Exact Mass: 510.3467

Molecular Weight: 511.62

Elemental Analysis: C, 58.69; H, 10.25; Cl, 13.86; N, 10.95; O, 6.25

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 460.00	2 Weeks

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Related CAS #

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Synonym

NPC-15437 hydrochloride; NPC-15437 HCl; N-161

IUPAC/Chemical Name

(2S)-2,6-diamino-N-[[1-(1-oxotridecyl)-2-piperidinyl]methyl]-hexanamide, dihydrochloride

InChi Key

RISSBZWRJRRXTD-OLBPYZPGSA-N

InChi Code

InChI=1S/C25H50N4O2.2ClH/c1-2-3-4-5-6-7-8-9-10-11-18-24(30)29-20-15-13-16-22(29)21-28-25(31)23(27)17-12-14-19-26;;/h22-23H,2-21,26-27H2,1H3,(H,28,31);2*1H/t22?,23-;;/m0../s1

SMILES Code

O=C(CCCCCCCCCCCC)N1CCCCC1CNC([C@@H](N)CCCCN)=O.Cl.Cl

Appearance

Solid powder

Purity

>95% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

NPC-15437 hydrochloride is a selective protein kinase C (PKC) inhibitor.

In vitro activity:

This study shows that an inhibitor with preference for novel PKC isozymes, NPC 15437, significantly augmented TRAIL sensitivity of A549 cells, as judged by assessing cell death and mitochondrial membrane potential. Likewise, NPC 15437 also significantly potentiated the responsiveness of DAOY medulloblastoma cells to TRAIL. Reference: Pathol Oncol Res. 2007;13(4):295-301. https://pubmed.ncbi.nlm.nih.gov/18158564/

In vivo activity:

This study aimed to determine the effect of cocaine pre-exposure on the acute and long-term effects of MDMA in mice. Co-administration of the protein kinase C (PKC) inhibitor NPC 15437 prevented cocaine protection. At the same time, after the course of cocaine, DAT density was reduced in the plasma membrane and increased in the endosome fraction, and this effect was prevented by NPC 15437. Reference: Br J Pharmacol. 2010 Jan;159(1):201-11. https://pubmed.ncbi.nlm.nih.gov/20015297/

	Solvent	mg/mL	mM
Solubility
	DMF	10.0	19.55
	DMSO	10.0	19.55
	Ethanol	5.0	9.77
	PBS (pH 7.2)	1.0	1.95

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 511.62 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Felber M, Sonnemann J, Beck JF. 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. doi: 10.1007/BF02940308. Epub 2007 Dec 25. PMID: 18158564. 2. Hsu KS, Huang CC. Protein kinase C inhibitors block generation of anoxia-induced long-term potentiation. Neuroreport. 1998 Oct 26;9(15):3525-9. doi: 10.1097/00001756-199810260-00035. PMID: 9855311. 3. Peraile I, Torres E, Mayado A, Izco M, Lopez-Jimenez A, Lopez-Moreno JA, Colado MI, O'Shea E. Dopamine transporter down-regulation following repeated cocaine: implications for 3,4-methylenedioxymethamphetamine-induced acute effects and long-term neurotoxicity in mice. Br J Pharmacol. 2010 Jan;159(1):201-11. doi: 10.1111/j.1476-5381.2009.00522.x. Epub 2009 Dec 10. PMID: 20015297; PMCID: PMC2823365. 4. Lai YT, Fan HY, Cherng CG, Chiang CY, Kao GS, Yu L. Activation of amygdaloid PKC pathway is necessary for conditioned cues-provoked cocaine memory performance. Neurobiol Learn Mem. 2008 Jul;90(1):164-70. doi: 10.1016/j.nlm.2008.03.006. Epub 2008 Apr 28. PMID: 18442936.

In vitro protocol:

In vivo protocol:

1. Peraile I, Torres E, Mayado A, Izco M, Lopez-Jimenez A, Lopez-Moreno JA, Colado MI, O'Shea E. Dopamine transporter down-regulation following repeated cocaine: implications for 3,4-methylenedioxymethamphetamine-induced acute effects and long-term neurotoxicity in mice. Br J Pharmacol. 2010 Jan;159(1):201-11. doi: 10.1111/j.1476-5381.2009.00522.x. Epub 2009 Dec 10. PMID: 20015297; PMCID: PMC2823365. 2. Lai YT, Fan HY, Cherng CG, Chiang CY, Kao GS, Yu L. Activation of amygdaloid PKC pathway is necessary for conditioned cues-provoked cocaine memory performance. Neurobiol Learn Mem. 2008 Jul;90(1):164-70. doi: 10.1016/j.nlm.2008.03.006. Epub 2008 Apr 28. PMID: 18442936.

1. Sullivan, J.P., Connor, J.R., Shearer, B.G., 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. 41(1), 38-44 (1992). 2. Mathis, C., Lehmann, J., and Ungerer, A. The selective protein kinase C inhibitor, NPC 15437, induces specific deficits in memory retention in mice. Eur. J. Pharmacol. 220(1), 107-110 (1992).