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

NPC-15437 hydrochloride
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 574806

CAS#: 141774-20-1

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

Chemical Structure

NPC-15437 hydrochloride

CAS# 141774-20-1

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 574806
Name: NPC-15437 hydrochloride
CAS#: 141774-20-1
Chemical Formula: C25H52Cl2N4O2
Exact Mass: 510.35
Molecular Weight: 511.617
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	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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:

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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/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. 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

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:	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.
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.

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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).

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