1. NF-κB
  2. Keap1-Nrf2 NF-κB
  3. Praelolide

Praelolide is a potent Nrf2 activator. Praelolide suppresses osteoclastogenesis and reactive oxygen species (ROS) production. Praelolide disrupts Keap1-Nrf2 protein-protein interactions by noncovalent binding to Keap1. Praelolide has the potential for the research of osteoclastogenic bone disease.

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Praelolide Chemical Structure

Praelolide Chemical Structure

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Description

Praelolide is a potent Nrf2 activator. Praelolide suppresses osteoclastogenesis and reactive oxygen species (ROS) production. Praelolide disrupts Keap1-Nrf2 protein-protein interactions by noncovalent binding to Keap1. Praelolide has the potential for the research of osteoclastogenic bone disease[1].

In Vitro

Praelolide (compound 21) (10 µM) shows anti-osteoclastogenesis activities with the inhibitory ratio of 100% in bone marrow monocytes/macrophages (BMMs)[1].
Praelolide (1, 1.25, 5, 10 µM; 1-5 days) inhibits RANKL-induced osteoclast formation with no cytotoxicity, and inhibits bone resorption of osteoclasts and actin ring formation in BMMs[1].
Praelolide (5, 10 µM) inhibits RANKL-induced mRNA levels of NFATc1, cathepsin K, MMP-9 and TRAP in BMMs[1].
Praelolide (5, 10 µM; 6 h) increases the protein expression of Nrf2, HO-1 and NQO1, enhances the stability of Nrf2 protein[1].
Praelolide (10 µM; 0-60 min) inhibits RANKL-induced NF-κB and MAPK signaling pathways and inhibits RANKL-induced phosphorylation of ERK, p38 MAPK, IKBα, and p65 NF-kB in pre-osteoclasts[1].
Praelolide (0, 20, 50, 100 µM; 24 h) interferes the interaction between Keap1 and Nrf2 by binding to Keap1 protein in RAW264.7 cells[1].

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

Cell Viability Assay[1]

Cell Line: Bone marrow monocytes/macrophages (BMMs)
Concentration: 1, 2.5, 5, 10, 20, 30, 40, 50 µM
Incubation Time: 1-5 days
Result: Suppressed RANKL-induced TRAP positive osteoclasts formation in a time dependent manner, shows no effect on cell viability.

RT-PCR[1]

Cell Line: Bone marrow monocytes/macrophages (BMMs)
Concentration: 5, 10 µM
Incubation Time: 1-5 days
Result: Inhibited RANKL-induced mRNA levels of NFATc1, cathepsin K, MMP-9 and TRAP.

Western Blot Analysis[1]

Cell Line: Bone marrow monocytes/macrophages (BMMs), RAW264.7 cells
Concentration: 5, 10 µM
Incubation Time: 6 h
Result: Promoted the protein expression of Nrf2 in the nucleus and HO-1 and NQO1 in the cytoplasm, ncreased the Nrf2 stability by reducing ubiquitin degradation of Nrf2.
In Vivo

Praelolide (2, 5, 10 µM; co-treated for 6 days) rescues the bone loss of prednisone-induced zebrafish[1].

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

Animal Model: Zebrafish larvae at the age of 3 dpf (day-post-fertilization)[1]
Dosage: 2, 5, 10 µM
Administration: Co-treated for 6 days
Result: Remarkably increased the amount of bone mineralization in prednisolone-treated zebrafish larvae especially at the concentration of 5 μM which even excelled 10 μM praelolide-treated group.
Molecular Weight

599.02

Formula

C28H35ClO12

SMILES

[H][C@@]1([C@H](OC(C)=O)[C@](O2)([C@H]3C)[C@@H](OC3=O)[C@H]4Cl)[C@@]([C@@H](OC(C)=O)CC[C@@]15OC5)(C)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]2C4=C

Structure Classification
Initial Source

Junceella juncea

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

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Praelolide
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HY-N10659
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