TBE56
TBE56, a molecular glue, is a BACH1 degrader, with an EC50 of 44 nM. TBE56 is a weak NRF2 inducer and the biotinylated TBE31. TBE56 interacts and promotes the degradation of BACH1 via a mechanism involving the E3 ligase FBX022. TBE56 reduces intracellular Fe2+ accumulation, ROS generation, and malondialdehyde (MDA) content, while increasing GSH/GSSG ratio and upregulating GPX4 in Prominin-2-overexpressed BMSCs. TBE56 significantly ameliorates intervertebral disc degeneration (IVDD) in puncture-induced SD rat IVDD model. TBE56 can be used for the study of intervertebral disc degeneration (IVDD).
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- Formule: C37H43N5O6S
- Masse moléculaire:685.83
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
TBE56 (100 nM, 3 h) significantly reduces BACH1 protein levels with an EC50 of 44 nM in HaCaT cells[1].
TBE56 (100 nM, 16 h) induces HMOX1 mRNA expression in HaCaT cells[1].
TBE56 (0.05-5 μM, 5-16 h) induces HMOX1 mRNA expression, promotes BACH1 degradation, and reduces nuclear BACH1 levels in A549, H1299, MDA-MB-231, and MDA-MB-468 cells in a concentration-dependent manner[1].
TBE56 (100 nM, 6 h) reduces migration and invasion of wild-type MDA-MB-231 cells[1].
TBE56 (110 nM, 3 h pretreatment) significantly decreases intracellular Fe2+ accumulation and ROS generation in Prominin-2-overexpressed BMSCs[2].
TBE56 (110 nM, 3 h pretreatment) significantly increases GSH/GSSG ratio and decreases MDA content in Prominin-2-overexpressed BMSCs[2].
TBE56 (110 nM, 16 h pretreatment) significantly improves viability and reduces LDH release in degenerative NPCs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HaCaT cells
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Concentration:100 nM
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Incubation Time:3 h
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Result:Reduced BACH1 protein levels with an EC50 of 44 nM in HaCaT cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Four-week-old male Sprague-Dawley (SD) rats (160–180 g): A needle was punctured into the center of lumbar IVD segments to induce disc degeneration, and SD rats’ forelimbs were amputated with the food trough raised post-surgery for 1-week recovery, establishing a puncture-induced SD rat IVDD model[1]
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Dosage:Pretreatment of Prominin-2-overexpressed BMSCs, 1×104 cells/μL, 10 μL per rat,
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Administration:Intradiscal injection, every 2 weeks for 2 months
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Result:Achieved enhanced retention of transplanted Prominin-2-overexpressed BMSCs in degenerated IVDs of SD rats.
Showed no significant changes in body weight.
Reduced the histological scores of IVD degeneration in SD rats.
Appeared elevated disc height index (DHI) percentage.
Showed greater amelioration of IVD degeneration with downregulated protein levels of MMP-9, ADAMTS5, and MMP-13 in degenerated IVD tissues of SD rats.
Achieved improved histological morphology of IVDs.
Reduced lipid peroxidation and oxidative stress in degenerated IVD microenvironment.
Chemical Information
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Masse moléculaire 685.83
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Formule C37H43N5O6S
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SMILES
C#C[C@@]12C([C@]3([C@]([C@](C)(C(C(C#N)=C3)=O)COC(CCCCCNC(CCCC[C@H]4[C@]5([H])[C@](NC(N5)=O)([H])CS4)=O)=O)([H])CC1)C)=CC(C(C#N)=C2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Moreno R, et al. Biotinylation of an acetylenic tricyclic bis(cyanoenone) lowers its potency as an NRF2 activator while creating a novel activity against BACH1. Free Radic Biol Med. 2022 Oct;191:203-211. [Content Brief]
[2]. Xu Y, et al. Prominin-2/FBXO22/BACH1 axis protects bone marrow mesenchymal stem cells against TBHP-induced ferroptosis and ameliorates intervertebral disc degeneration. Stem Cell Res Ther. 2025 Jul 1;16(1):340. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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