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