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  3. TBE56

TBE56,一种分子胶, 是一种 BACH1 降解剂,其 EC50 为 44 nM。TBE56 是一种弱 NRF2 诱导剂,也是生物素化的 TBE31。TBE56 通过一种涉及 E3 连接酶 FBX022 的机制与 BACH1 相互作用并促进其降解。TBE56 可减少 Prominin-2 过表达的骨髓间充质干细胞 (BMSCs) 中 Fe2+ 的累积、ROS 的生成及丙二醛 (MDA) 含量,同时提高 GSH/GSSG 比值并上调 GPX4。TBE56 在穿刺诱导的 SD 大鼠椎间盘退变 (IVDD) 模型中可显著改善椎间盘退变。TBE56 可用于椎间盘退变 (IVDD) 的研究。

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TBE56

TBE56 Chemical Structure

CAS No. : 1459836-79-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)[1][2].

体外研究
(In Vitro)

TBE56 (100 nM, 3 h) 可显著降低 HaCaT 细胞中 BACH1 蛋白水平,EC50 为 44 nM[1]
TBE56 (100 nM, 16 h) 可诱导 HaCaT 细胞中 HMOX1 mRNA 表达[1]
TBE56 (0.05-5 μM, 5-16 h) 可诱导 A549、H1299、MDA-MB-231 和 MDA-MB-468 细胞中 HMOX1 mRNA 表达,促进 BACH1 降解,并降低核内 BACH1 水平,且呈浓度依赖性[1]
TBE56 (100 nM, 6 h) 可降低野生型 MDA-MB-231 细胞的迁移和侵袭能力[1]
TBE56 (110 nM, 3 h 预处理) 可显著减少 Prominin-2-overexpressed BMSCs 中 Fe2+ 的累积及 ROS 生成[2]
TBE56 (110 nM, 3 h 预处理) 可显著提高 Prominin-2-overexpressed BMSCs 的 GSH/GSSG 比值,并降低 MDA 含量[2]
TBE56 (110 nM, 16 h 预处理) 可显著改善 degenerative NPCs 的活力并减少 LDH 释放[2]

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

Western Blot Analysis[1]

Cell Line: HaCaT cells
Concentration: 100 nM
Incubation Time: 3 h
Result: Reduced BACH1 protein levels with an EC50 of 44 nM in HaCaT cells.
体内研究
(In Vivo)

TBE56 (对过表达 Prominin-2 的骨髓间充质干细胞(BMSCs)预处理,1×104 cells/μL,10 μL/只大鼠,椎间盘内注射,每两周一次,共 2 个月) 可显著改善穿刺诱导的 SD 大鼠椎间盘退变(IVDD)模型[1]

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

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]
Dosage: Pretreatment of Prominin-2-overexpressed BMSCs, 1×104 cells/μL, 10 μL per rat,
Administration: Intradiscal injection, every 2 weeks for 2 months
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.
分子量

685.83

Formula

C37H43N5O6S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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  • 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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TBE56
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HY-17655
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