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non-electrophilic nrf2 activators 6  (Sanofi)

 
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    Structured Review

    Sanofi non-electrophilic nrf2 activators 6
    Under basal conditions, <t>NRF2</t> is bound to KEAP1, ubiquitinated by CUL3, and degraded by the proteasome (top). In the presence of an electrophile (middle) or a non-covalent inhibitor (bottom), NRF2 translocates to the nucleus and transcribes cytoprotective genes, like NADPH quinone oxidoreductase 1 (NQO1), heme oxygenase-1 (HO-1), and glutathione S-transferase (GST).
    Non Electrophilic Nrf2 Activators 6, supplied by Sanofi, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/product/nrf2+activators+6/nrf2+activators+6/pmc07315935-54-4-13
    Average 90 stars, based on 1 article reviews
    non-electrophilic nrf2 activators 6 - by Bioz Stars, 2026-09
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    Images

    1) Product Images from "Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability"

    Article Title: Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability

    Journal: Journal of medicinal chemistry

    doi: 10.1021/acs.jmedchem.9b01074

    Under basal conditions, NRF2 is bound to KEAP1, ubiquitinated by CUL3, and degraded by the proteasome (top). In the presence of an electrophile (middle) or a non-covalent inhibitor (bottom), NRF2 translocates to the nucleus and transcribes cytoprotective genes, like NADPH quinone oxidoreductase 1 (NQO1), heme oxygenase-1 (HO-1), and glutathione S-transferase (GST).
    Figure Legend Snippet: Under basal conditions, NRF2 is bound to KEAP1, ubiquitinated by CUL3, and degraded by the proteasome (top). In the presence of an electrophile (middle) or a non-covalent inhibitor (bottom), NRF2 translocates to the nucleus and transcribes cytoprotective genes, like NADPH quinone oxidoreductase 1 (NQO1), heme oxygenase-1 (HO-1), and glutathione S-transferase (GST).

    Techniques Used:

    IC 50 , logD 7.4 , and Metabolic t 1/2 of Isoquinoline NRF2 Activators
    Figure Legend Snippet: IC 50 , logD 7.4 , and Metabolic t 1/2 of Isoquinoline NRF2 Activators

    Techniques Used:

    A) HaCaT cells were treated with vehicle control DMSO, 10 μM compound (5e, 12, 5a, 11b, 11c, 13a), or positive control 3 (1 μM) for 16 h. Cell lysates were prepared, equal amounts of protein was probed with antibodies specific for NRF2 or NQO1. Actin was used as a reference. Image was cropped at the dotted line to remove an unrelated compound. See the supplemental information for the uncropped images. NRF2 and NQO1 band intensities were quantified using NIH ImageJ software, and were normalized to that of respective actin band intensity. The normalized values of NRF2 and NQO1 of DMSO-treated samples was taken as one unit. The fold increase in NRF2 and NQO1 expression of two independent sets is presented relative to DMSO controls independently or combined. B) HaCaT cells were treated with DMSO, 0.1, 1, or 10 μM 13a, or 250 nM 3.
    Figure Legend Snippet: A) HaCaT cells were treated with vehicle control DMSO, 10 μM compound (5e, 12, 5a, 11b, 11c, 13a), or positive control 3 (1 μM) for 16 h. Cell lysates were prepared, equal amounts of protein was probed with antibodies specific for NRF2 or NQO1. Actin was used as a reference. Image was cropped at the dotted line to remove an unrelated compound. See the supplemental information for the uncropped images. NRF2 and NQO1 band intensities were quantified using NIH ImageJ software, and were normalized to that of respective actin band intensity. The normalized values of NRF2 and NQO1 of DMSO-treated samples was taken as one unit. The fold increase in NRF2 and NQO1 expression of two independent sets is presented relative to DMSO controls independently or combined. B) HaCaT cells were treated with DMSO, 0.1, 1, or 10 μM 13a, or 250 nM 3.

    Techniques Used: Control, Positive Control, Software, Expressing

    Quantification of Western Blot Data in Figure 3A .
    Figure Legend Snippet: Quantification of Western Blot Data in Figure 3A .

    Techniques Used: Western Blot

    Quantification of Western Blot Data in Figure 3B .
    Figure Legend Snippet: Quantification of Western Blot Data in Figure 3B .

    Techniques Used: Western Blot

    Related Articles

    other:

    Article Title: Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability
    Article Snippet: 19-20 Other non-electrophilic NRF2 activators have been reported by groups at Sanofi (6) 21 and GlaxoSmithKline/Astex (7) 22-23 and are shown in Chart 2.



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    non-electrophilic nrf2 activators 6  (Sanofi)
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    Sanofi non-electrophilic nrf2 activators 6
    Under basal conditions, <t>NRF2</t> is bound to KEAP1, ubiquitinated by CUL3, and degraded by the proteasome (top). In the presence of an electrophile (middle) or a non-covalent inhibitor (bottom), NRF2 translocates to the nucleus and transcribes cytoprotective genes, like NADPH quinone oxidoreductase 1 (NQO1), heme oxygenase-1 (HO-1), and glutathione S-transferase (GST).
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    nrf2 activators 6  (Sanofi)
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    Sanofi nrf2 activators 6
    Under basal conditions, <t>NRF2</t> is bound to KEAP1, ubiquitinated by CUL3, and degraded by the proteasome (top). In the presence of an electrophile (middle) or a non-covalent inhibitor (bottom), NRF2 translocates to the nucleus and transcribes cytoprotective genes, like NADPH quinone oxidoreductase 1 (NQO1), heme oxygenase-1 (HO-1), and glutathione S-transferase (GST).
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    https://www.bioz.com/product/nrf2+activators+6/nrf2+activators+6/10__1021_slash_acs__jmedchem__9b01074-40-2-11
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    Image Search Results


    Under basal conditions, NRF2 is bound to KEAP1, ubiquitinated by CUL3, and degraded by the proteasome (top). In the presence of an electrophile (middle) or a non-covalent inhibitor (bottom), NRF2 translocates to the nucleus and transcribes cytoprotective genes, like NADPH quinone oxidoreductase 1 (NQO1), heme oxygenase-1 (HO-1), and glutathione S-transferase (GST).

    Journal: Journal of medicinal chemistry

    Article Title: Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability

    doi: 10.1021/acs.jmedchem.9b01074

    Figure Lengend Snippet: Under basal conditions, NRF2 is bound to KEAP1, ubiquitinated by CUL3, and degraded by the proteasome (top). In the presence of an electrophile (middle) or a non-covalent inhibitor (bottom), NRF2 translocates to the nucleus and transcribes cytoprotective genes, like NADPH quinone oxidoreductase 1 (NQO1), heme oxygenase-1 (HO-1), and glutathione S-transferase (GST).

    Article Snippet: 19 – 20 Other non-electrophilic NRF2 activators have been reported by groups at Sanofi ( 6 ) 21 and GlaxoSmithKline/Astex ( 7 ) 22 – 23 and are shown in .

    Techniques:

    IC 50 , logD 7.4 , and Metabolic t 1/2 of Isoquinoline NRF2 Activators

    Journal: Journal of medicinal chemistry

    Article Title: Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability

    doi: 10.1021/acs.jmedchem.9b01074

    Figure Lengend Snippet: IC 50 , logD 7.4 , and Metabolic t 1/2 of Isoquinoline NRF2 Activators

    Article Snippet: 19 – 20 Other non-electrophilic NRF2 activators have been reported by groups at Sanofi ( 6 ) 21 and GlaxoSmithKline/Astex ( 7 ) 22 – 23 and are shown in .

    Techniques:

    A) HaCaT cells were treated with vehicle control DMSO, 10 μM compound (5e, 12, 5a, 11b, 11c, 13a), or positive control 3 (1 μM) for 16 h. Cell lysates were prepared, equal amounts of protein was probed with antibodies specific for NRF2 or NQO1. Actin was used as a reference. Image was cropped at the dotted line to remove an unrelated compound. See the supplemental information for the uncropped images. NRF2 and NQO1 band intensities were quantified using NIH ImageJ software, and were normalized to that of respective actin band intensity. The normalized values of NRF2 and NQO1 of DMSO-treated samples was taken as one unit. The fold increase in NRF2 and NQO1 expression of two independent sets is presented relative to DMSO controls independently or combined. B) HaCaT cells were treated with DMSO, 0.1, 1, or 10 μM 13a, or 250 nM 3.

    Journal: Journal of medicinal chemistry

    Article Title: Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability

    doi: 10.1021/acs.jmedchem.9b01074

    Figure Lengend Snippet: A) HaCaT cells were treated with vehicle control DMSO, 10 μM compound (5e, 12, 5a, 11b, 11c, 13a), or positive control 3 (1 μM) for 16 h. Cell lysates were prepared, equal amounts of protein was probed with antibodies specific for NRF2 or NQO1. Actin was used as a reference. Image was cropped at the dotted line to remove an unrelated compound. See the supplemental information for the uncropped images. NRF2 and NQO1 band intensities were quantified using NIH ImageJ software, and were normalized to that of respective actin band intensity. The normalized values of NRF2 and NQO1 of DMSO-treated samples was taken as one unit. The fold increase in NRF2 and NQO1 expression of two independent sets is presented relative to DMSO controls independently or combined. B) HaCaT cells were treated with DMSO, 0.1, 1, or 10 μM 13a, or 250 nM 3.

    Article Snippet: 19 – 20 Other non-electrophilic NRF2 activators have been reported by groups at Sanofi ( 6 ) 21 and GlaxoSmithKline/Astex ( 7 ) 22 – 23 and are shown in .

    Techniques: Control, Positive Control, Software, Expressing

    Quantification of Western Blot Data in Figure 3A .

    Journal: Journal of medicinal chemistry

    Article Title: Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability

    doi: 10.1021/acs.jmedchem.9b01074

    Figure Lengend Snippet: Quantification of Western Blot Data in Figure 3A .

    Article Snippet: 19 – 20 Other non-electrophilic NRF2 activators have been reported by groups at Sanofi ( 6 ) 21 and GlaxoSmithKline/Astex ( 7 ) 22 – 23 and are shown in .

    Techniques: Western Blot

    Quantification of Western Blot Data in Figure 3B .

    Journal: Journal of medicinal chemistry

    Article Title: Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability

    doi: 10.1021/acs.jmedchem.9b01074

    Figure Lengend Snippet: Quantification of Western Blot Data in Figure 3B .

    Article Snippet: 19 – 20 Other non-electrophilic NRF2 activators have been reported by groups at Sanofi ( 6 ) 21 and GlaxoSmithKline/Astex ( 7 ) 22 – 23 and are shown in .

    Techniques: Western Blot