NK-252 | CAS#1414963-82-8 | Nrf2 activator

NK-252
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 562438

CAS#: 1414963-82-8

Description: NK-252 is a Nrf2 activator. It acts by interacting with the Nrf2-binding site of Keap1 and downregulates the expression of fibrogenic genes.

Chemical Structure

NK-252

CAS# 1414963-82-8

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 562438
Name: NK-252
CAS#: 1414963-82-8
Chemical Formula: C13H11N5O3
Exact Mass: 285.09
Molecular Weight: 285.263
Elemental Analysis: C, 54.74; H, 3.89; N, 24.55; O, 16.83

Price and Availability

Size	Price	Availability
10mg	USD 450	2 Weeks
25mg	USD 750	2 Weeks
100mg	USD 1650	2 Weeks
1g	USD 4650	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: NK-252; NK 252; NK252;

IUPAC/Chemical Name: N-[5-(2-Furanyl)-1,3,4-oxadiazol-2-yl]-N-(2-pyridinylmethyl)urea

InChi Key: LEATYIHSFPWADP-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H11N5O3/c14-12(19)18(8-9-4-1-2-6-15-9)13-17-16-11(21-13)10-5-3-7-20-10/h1-7H,8H2,(H2,14,19)

SMILES Code: O=C(N)N(C1=NN=C(C2=CC=CO2)O1)CC3=NC=CC=C3

Appearance: Solid powder

Purity: >98% (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: >2 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:	NK-252 is a Nrf2 activator.
In vitro activity:	The aim of the present study was to investigate whether oxaliplatin could exert anticancer effects on CRC by promoting ferroptosis and oxidative stress. Furthermore, after treating cells with the Nrf2 activator, NK-252, Fe2+ was detected in cells using a commercial kit. Reference: Exp Ther Med. 2022 Jun;23(6):394. doi: 10.3892/etm.2022.11321. https://pubmed.ncbi.nlm.nih.gov/35495610/
In vivo activity:	For in vivo animal model studies, we used rats on a choline-deficient L-amino acid-defined (CDAA) diet, which demonstrate pathologic findings similar to those seen in human NASH. The administration of OPZ or NK-252 significantly attenuated the progression of histologic abnormalities in rats on a CDAA diet, especially hepatic fibrosis. Reference: Mol Pharmacol. 2013 Jul;84(1):62-70. https://pubmed.ncbi.nlm.nih.gov/23592516/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	20.0	70.11
	DMF:PBS (pH 7.2) (1:1)	0.5	1.75
	DMSO	23.8	83.58

Preparing Stock Solutions

The following data is based on the product molecular weight 285.26 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. Liu B, Wang H. Oxaliplatin induces ferroptosis and oxidative stress in HT29 colorectal cancer cells by inhibiting the Nrf2 signaling pathway. Exp Ther Med. 2022 Jun;23(6):394. doi: 10.3892/etm.2022.11321. Epub 2022 Apr 13. PMID: 35495610; PMCID: PMC9047032. 2. Kiue A, Sano T, Naito A, Inada H, Suzuki K, Okumura M, Kikuchi J, Sato S, Takano H, Kohno K, et al. Reversal by two dihydropyridine compounds of resistance to multiple anticancer agents in mouse P388 leukemia in vivo and in vitro. Jpn J Cancer Res. 1990 Oct;81(10):1057-64. doi: 10.1111/j.1349-7006.1990.tb03346.x. PMID: 1977728; PMCID: PMC5917977. 3. Shi Y, Sun Y, Sun X, Zhao H, Yao M, Hou L, Jiang L. Up-regulation of HO-1 by Nrf2 activation protects against palmitic acid-induced ROS increase in human neuroblastoma BE(2)-M17 cells. Nutr Res. 2018 Apr;52:80-86. doi: 10.1016/j.nutres.2018.02.003. Epub 2018 Feb 12. PMID: 29526395. 4. Shimozono R, Asaoka Y, Yoshizawa Y, Aoki T, Noda H, Yamada M, Kaino M, Mochizuki H. Nrf2 activators attenuate the progression of nonalcoholic steatohepatitis-related fibrosis in a dietary rat model. Mol Pharmacol. 2013 Jul;84(1):62-70. doi: 10.1124/mol.112.084269. Epub 2013 Apr 16. PMID: 23592516.
In vitro protocol:	1. Liu B, Wang H. Oxaliplatin induces ferroptosis and oxidative stress in HT29 colorectal cancer cells by inhibiting the Nrf2 signaling pathway. Exp Ther Med. 2022 Jun;23(6):394. doi: 10.3892/etm.2022.11321. Epub 2022 Apr 13. PMID: 35495610; PMCID: PMC9047032. 2. Kiue A, Sano T, Naito A, Inada H, Suzuki K, Okumura M, Kikuchi J, Sato S, Takano H, Kohno K, et al. Reversal by two dihydropyridine compounds of resistance to multiple anticancer agents in mouse P388 leukemia in vivo and in vitro. Jpn J Cancer Res. 1990 Oct;81(10):1057-64. doi: 10.1111/j.1349-7006.1990.tb03346.x. PMID: 1977728; PMCID: PMC5917977.
In vivo protocol:	1. Shi Y, Sun Y, Sun X, Zhao H, Yao M, Hou L, Jiang L. Up-regulation of HO-1 by Nrf2 activation protects against palmitic acid-induced ROS increase in human neuroblastoma BE(2)-M17 cells. Nutr Res. 2018 Apr;52:80-86. doi: 10.1016/j.nutres.2018.02.003. Epub 2018 Feb 12. PMID: 29526395. 2. Shimozono R, Asaoka Y, Yoshizawa Y, Aoki T, Noda H, Yamada M, Kaino M, Mochizuki H. Nrf2 activators attenuate the progression of nonalcoholic steatohepatitis-related fibrosis in a dietary rat model. Mol Pharmacol. 2013 Jul;84(1):62-70. doi: 10.1124/mol.112.084269. Epub 2013 Apr 16. PMID: 23592516.

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1: Shi Y, Sun Y, Sun X, Zhao H, Yao M, Hou L, Jiang L. Up-regulation of HO-1 by Nrf2 activation protects against palmitic acid-induced ROS increase in human neuroblastoma BE(2)-M17 cells. Nutr Res. 2018 Feb 12. pii: S0271-5317(17)30819-9. doi: 10.1016/j.nutres.2018.02.003. [Epub ahead of print] PubMed PMID: 29526395.

2: Shimozono R, Asaoka Y, Yoshizawa Y, Aoki T, Noda H, Yamada M, Kaino M, Mochizuki H. Nrf2 activators attenuate the progression of nonalcoholic steatohepatitis-related fibrosis in a dietary rat model. Mol Pharmacol. 2013 Jul;84(1):62-70. doi: 10.1124/mol.112.084269. Epub 2013 Apr 16. PubMed PMID: 23592516.

3: Saito T, Hikita M, Kohno K, Sato S, Takano H, Kobayashi M. Different sensitivities of human esophageal cancer cells to multiple anti-cancer agents and related mechanisms. Cancer. 1992 Nov 15;70(10):2402-9. PubMed PMID: 1358426.

4: Kiue A, Sano T, Naito A, Okumura M, Kohno K, Kuwano M. Enhancement of antitumour activity of etoposide by dihydropyridines on drug-sensitive and drug-resistant leukaemia in mice. Br J Cancer. 1991 Aug;64(2):221-6. PubMed PMID: 1892749; PubMed Central PMCID: PMC1977534.

5: Watanabe Y, Takano H, Kiue A, Kohno K, Kuwano M. Potentiation of etoposide and vincristine by two synthetic 1,4-dihydropyridine derivatives in multidrug-resistant and atypical multidrug-resistant human cancer cells. Anticancer Drug Des. 1991 Feb;6(1):47-57. PubMed PMID: 2015041.

6: Kiue A, Sano T, Naito A, Inada H, Suzuki K, Okumura M, Kikuchi J, Sato S, Takano H, Kohno K, et al. Reversal by two dihydropyridine compounds of resistance to multiple anticancer agents in mouse P388 leukemia in vivo and in vitro. Jpn J Cancer Res. 1990 Oct;81(10):1057-64. PubMed PMID: 1977728.

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