| Chemical Properties | Back Directory | [Boiling point ]
752.2±70.0 °C(Predicted) | [density ]
1.357±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 10mg/mL, clear | [form ]
Solid | [pka]
8.33±0.30(Predicted) | [color ]
Off-white to light yellow | [InChIKey]
VUIVGOOWLHGDPZ-UHFFFAOYSA-N | [SMILES]
CC(CC1=C(NS(C2=CC=C(OCC)C=C2)(=O)=O)C3=C(C=CC=C3)C(NS(C4=CC=C(OCC)C=C4)(=O)=O)=C1)=O |
| Hazard Information | Back Directory | [Description]
K67 is a specific inhibitor against the interaction between KEAP1 DC domain and S349-phosphorylated KIR of p62/SQSTM1, K67 effectively inhibits the proliferation of HCC cultures with high cellular p62 S351-phosphorylation by restoring KEAP1-driven NRF2 ubiquitination and degradation. | [Uses]
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]. | [References]
[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. DOI:10.1038/ncomms12030
[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. DOI:10.1016/j.bmcl.2016.10.083 |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|