2046250-48-8
Chemical Structure
K67
- CAS 番号: 2046250-48-8
- Formula:C29H30N2O7S2
- Molecular Weight:582.69
IUPAC Name: N,N'-(2-(2-oxopropyl)naphthalene-1,4-diyl)bis(4-ethoxybenzenesulfonamide)
InChIKey: VUIVGOOWLHGDPZ-UHFFFAOYSA-N
SMILES: CC(CC1=CC(NS(C2=CC=C(C=C2)OCC)(=O)=O)=C3C=CC=CC3=C1NS(C4=CC=C(C=C4)OCC)(=O)=O)=O
Biological Activity: K67 is a selective the interaction between Keap1 and S349 phosphorylated p62 inhibitor, with an IC50 of 1.5 μM. K67 has a weaker inhibitory effect on the interaction between Keap1 and Nrf2 (IC50 is 6.2 μM). K67 competitively binds to the binding site of Keap1 with p-p62, blocking the abnormal activation of the p62-dependent Nrf2 pathway. K67 inhibits tumor cell proliferation and enhances the sensitivity of hepatocellular carcinoma (HCC) to chemotherapeutic drugs by restoring Keap1-mediated ubiquitination and degradation of Nrf2[1][2].
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K67 | 98.26% | K67 is a selective the interaction between Keap1 and S349 phosphorylated p62 inhibitor, with an IC50 of 1.5 μM. K67 has a weaker inhibitory effect on the interaction between Keap1 and Nrf2 (IC50 is 6.2 μM). K67 competitively binds to the binding site of Keap1 with p-p62, blocking the abnormal activation of the p62-dependent Nrf2 pathway. K67 inhibits tumor cell proliferation and enhances the sensitivity of hepatocellular carcinoma (HCC) to chemotherapeutic drugs by restoring Keap1-mediated ubiquitination and degradation of Nrf2. | ||||||||||||||||||||
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- [1]. Saito T, et al. p62/Sqstm1 promotes malignancy of HCV-positive hepatocellular carcinoma through Nrf2-dependent metabolic reprogramming. Nat Commun. 2016 Jun 27;7:12030. [Content Brief]
- [2]. Yasuda D, et al. Synthesis of Keap1-phosphorylated p62 and Keap1-Nrf2 protein-protein interaction inhibitors and their inhibitory activity. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5956-5959. [Content Brief]
Keywords
