2. NF-κB MAPK/ERK Pathway
  3. Keap1-Nrf2 NF-κB p38 MAPK
  4. Nrf2 activator-23

Nrf2 activator-23 is an orally active Keap1 binder and Nrf2 activator, with KD values of 28.68 nM and 54.55 nM for Keap1 and its Kelch domain, respectively. Nrf2 activator-23 disrupts the Keap1-Nrf2 interaction, reduces ubiquitination and degradation of Nrf2, and activates the Nrf2 signaling pathway. Nrf2 activator-23 inhibits RANKL-induced osteoclast formation, bone resorptive activity, ROS production, and activation of the MAPK and NF-κB signaling pathways, while downregulating the expression of osteoclast-specific genes and proteins. Nrf2 activator-23 attenuates bone loss and reduces osteoclast formation in vivo without affecting osteoblast differentiation and mineralization. Nrf2 activator-23 can be used for the research of osteoporosis.

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Nrf2 activator-23

Nrf2 activator-23 Chemical Structure

CAS No. : 3109883-60-2

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Nrf2 activator-23 Related Antibodies

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Description

Nrf2 activator-23 is an orally active Keap1 binder and Nrf2 activator, with KD values of 28.68 nM and 54.55 nM for Keap1 and its Kelch domain, respectively. Nrf2 activator-23 disrupts the Keap1-Nrf2 interaction, reduces ubiquitination and degradation of Nrf2, and activates the Nrf2 signaling pathway. Nrf2 activator-23 inhibits RANKL-induced osteoclast formation, bone resorptive activity, ROS production, and activation of the MAPK and NF-κB signaling pathways, while downregulating the expression of osteoclast-specific genes and proteins. Nrf2 activator-23 attenuates bone loss and reduces osteoclast formation in vivo without affecting osteoblast differentiation and mineralization. Nrf2 activator-23 can be used for the research of osteoporosis[1].

In Vitro

Nrf2 activator-23 (compound 5c) (1 μM; 4-7 d) inhibits RANKL-induced osteoclast differentiation in RAW264.7 cells, with an IC50 of 0.499 μM after 7 days of treatment[1].
Nrf2 activator-23 (0.5-2 μM; 7 d) dose-dependently disrupts the formation of F-actin rings, reduces osteoclast volume, and decreases the number of nuclei per osteoclast in RANKL-stimulated bone marrow macrophages (BMMs) after 7 days of treatment[1].
Nrf2 activator-23 (0.5-2 μM; 7 d) inhibits RANKL-stimulated bone resorption by BMMs in a dose-dependent manner, and achieves nearly complete inhibition at the concentration of 2 μM after 7 days of treatment[1].
Nrf2 activator-23 (0.5-2 μM; 7 d) dose-dependently downregulates the mRNA expression levels of key genes (C-Fos, MMP-9, TRAP, NFATc1, CTSK, DC-STAMP) associated with osteoclast differentiation and function in RANKL-stimulated BMMs[1].
Nrf2 activator-23 (0.5-2 μM; 4 d) dose-dependently downregulates the protein expression of key markers for osteoclast differentiation and function (NFATc1, MMP-9, C-Fos, CTSK) in RANKL-stimulated bone marrow-derived macrophages (BMMs)[1].
Nrf2 activator-23 (0.5-2 μM; 48 h) inhibits RANKL-induced intracellular and mitochondrial ROS production in bone marrow macrophages (BMMs) in a dose-dependent manner, with a treatment duration of 48 h[1].
Nrf2 activator-23 (1 μM; 48 h) reduces the ubiquitination level of Nrf2 in BMMs and inhibits its proteasomal degradation[1].
Nrf2 activator-23 (1 μM; 6 h) inhibits the activation of MAPK (p38, ERK, JNK) and NF-κB (p65, IκBα) signaling pathways in RANKL-induced BMMs after 6 h of pretreatment[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Nrf2 activator-23 Related Antibodies

Real Time qPCR[1]

Cell Line: RANKL-induced mouse bone marrow macrophages (BMMs)
Concentration: 0.5-2 μM
Incubation Time: ~7 days (until osteoclast formation)
Result: Dose-dependently reduced the mRNA expression of all tested osteoclast-specific genes.
Reduced C-Fos, MMP-9, TRAP, NFATc1, and CTSK expression to <20% of the RANKL-induced control, and DC-STAMP expression to ~30% of the control at 2 μM.

Western Blot Analysis[1]

Cell Line: RANKL-induced mouse bone marrow macrophages (BMMs)
Concentration: 0.5-2 μM
Incubation Time: 4 days
Result: Dose-dependently reduced the protein expression of NFATc1, MMP-9, C-Fos, and CTSK compared to the RANKL-induced control.
Reduced NFATc1 and C-Fos expression to <50% of the control, and MMP-9 and CTSK expression to ~40% of the control at 2 μM.

Western Blot Analysis[1]

Cell Line: RANKL-induced mouse bone marrow macrophages (BMMs)
Concentration: 1 μM
Incubation Time: 6 h pre-incubation, followed by RANKL stimulation for up to 60 min
Result: Attenuated RANKL-induced phosphorylation of p38, ERK, JNK, p65, and IκBα in a time-dependent manner.
Reduced p38, ERK, and JNK phosphorylation to ~60-70% of the control, and p65 and IκBα phosphorylation to ~50-60% of the control at 10 min post-RANKL stimulation.
Parmacokinetics
Species Dose Route AUC0-t Cmax T1/2 Bioavailability
Mice[1] 10 mg/kg p.o. 5069 ng·h/mL 223 ng/mL >24 h 9.4 %
In Vivo

Nrf2 activator-23 (compound 5c) (10 mg/kg; p.o.; administered once every other day for 8 consecutive weeks) effectively alleviates ovariectomy-induced bone loss in female C57BL/6J mice, with efficacy comparable to that of Alendronate sodium hydrate (HY-11101)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (7-week-old female, ovariectomized)[1]
Dosage: 10 mg/kg
Administration: p.o.; every other day; 8 weeks
Result: Increased bone volume/total bone volume (BV/TV), trabecular number (Tb.N), and trabecular thickness (Tb.Th), while decreasing trabecular spacing (Tb.Sp) compared to OVX controls.
Prevented the decrease in bone surface (BS) caused by ovariectomy.
Markedly reduced the increase in osteoclast surface/bone surface (Oc.S/BS) ratio induced by OVX.
Promoted gene expression of Nfe2l2 and Cat.
Showed no obvious toxicity, with no differences in body weight or organ histology (heart, liver, spleen, lung, kidney).
Molecular Weight

423.34

Formula

C23H17FO2Se
CAS No.
SMILES

O=C1C=C(OC2=CC(F)=CC([Se]C3=CC(C)=CC=C3)=C21)C4=CC=CC(C)=C4
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Purity & Documentation
References
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Nrf2 activator-23 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nrf2 activator-233109883-60-2Keap1-Nrf2NF-κBp38 MAPKNuclear factor-κBNuclear factor-kappaBosteoporosisosteoblastsNrf2 signaling pathwayKelch domainKeap1osteoclastsRAW264.7 cellsBMMsRANKLNrf2Inhibitorinhibitorinhibit

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