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Necrox-5 methanesulfonate

Names

[ CAS No. ]:
1383718-29-3

[ Name ]:
Necrox-5 methanesulfonate

[Synonym ]:
1H-Indol-7-amine, 5-[(1,1-dioxido-4-thiomorpholinyl)methyl]-2-phenyl-N-[(tetrahydro-2H-pyran-4-yl)methyl]-, methanesulfonate (1:2)
5-[(1,1-Dioxido-4-thiomorpholinyl)methyl]-2-phenyl-N-(tetrahydro-2H-pyran-4-ylmethyl)-1H-indol-7-amine methanesulfonate (1:2)

Biological Activity

[Description]:

NecroX-5 is a derivative of the NecroX, reduces intracellular calcium concentration, and possesses anti-inflammatory and anti-cancer activity.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel
Research Areas >> Cancer
Research Areas >> Inflammation/Immunology

[Target]

Calcium channel[1]


[In Vitro]

NecroX-5 (10 or 40 μM) inhibits breast cancer cell migration, which is correlated with mitoROS reduction, and mediated by AKT inhibition. NecroX-5 (10 μM) decreases intracellular calcium concentration in 4T1 cells by blocking Ca2+ influx, which mediated the inhibition of cell migration, AKT downregulation and the reduction of mitochondrial ROS levels[1]. NecroX-5 (10 µM) treatment for 24 h, effectively decreases the increased TNFα, TGFβ1, pSmad2 and the expression of Dcn in LPS-stimulated H9C2 cells[2].

[In Vivo]

NecroX-5 (2.5 mg/kg, everyday other day) inhibits breast cancer cell metastasis in TUBO-P2J tumour-bearing mice[1].

[References]

[1]. Park JH, et al. NecroX-5 prevents breast cancer metastasis by AKT inhibition via reducing intracellular calcium levels. Int J Oncol. 2017 Jan;50(1):185-192.

[2]. Thu VT, et al. NecroX-5 exerts anti-inflammatory and anti-fibrotic effects via modulation of the TNFα/Dcn/TGFβ1/Smad2 pathway in hypoxia/reoxygenation-treated rat hearts. Korean J Physiol Pharmacol. 2016 May;20(3):305-14.


[Related Small Molecules]

Neomycin sulfate | Nifedipine | Acetylcholine chloride | Ionomycin | (S)-(-)-Bay K 8644 | Nimodipine | Mibefradil dihydrochloride | Levetiracetam | CDN 1163 | Dantrolene sodium | Thapsigargin | Flufenamic Acid | ABT 639 | Ranolazine dihydrochloride | Cromolyn (sodium)

Chemical & Physical Properties

[ Molecular Formula ]:
C27H39N3O9S3

[ Molecular Weight ]:
645.808

[ Exact Mass ]:
645.184814

[ Storage condition ]:
2-8℃

Related Compounds