2. PROTAC Cell Cycle/DNA Damage
  3. DUBTACs Deubiquitinase
  4. FXR DUBTAC IN-1

FXR DUBTAC IN-1 (compound D11) 是一种靶向 FXR 的去泛素酶靶向嵌合体 (DUBTAC)，对 FXR 的 Ka 值为 2.12e-5 M。FXR DUBTAC IN-1 可招募去泛素化酶 OTUB1，与 OTUB1 结合并和 FXR 形成三元复合物，降低 FXR 的多泛素化水平，通过泛素-蛋白酶体通路阻止 FXR 降解，并提升 FXR 的蛋白水平。FXR DUBTAC IN-1 可用于胆汁淤积性肝损伤的研究。

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FXR DUBTAC IN-1

FXR DUBTAC IN-1 Chemical Structure

CAS No. : 3081876-96-9

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FXR DUBTAC IN-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FXR DUBTAC IN-1 (compound D11) is a deubiquitinase-targeting chimeric molecule (DUBTAC) that targets FXR, with a Ka value of 2.12e-5 M for FXR. FXR DUBTAC IN-1 recruits the deubiquitinase OTUB1, binds to OTUB1 and forms a ternary complex with FXR, reduces the polyubiquitination level of FXR, prevents FXR degradation via the ubiquitin-proteasome pathway, and elevates the protein level of FXR. FXR DUBTAC IN-1 can be used in the research of cholestatic liver injury[1].

体外研究
(In Vitro)

FXR DUBTAC IN-1 (compound D11) (1-10 μM; 24 h) 可显著上调 HepG2 细胞中 FXR 蛋白的表达，且在 50 μM 浓度下仍能维持 70.71% 的细胞存活率[1]。
FXR DUBTAC IN-1 (0.1-10 μM) 以剂量依赖的方式上调 HepG2 细胞中的 FXR 蛋白水平[1]。
FXR DUBTAC IN-1 (1 μM; 1-8 h) 以时间依赖的方式上调 HepG2 细胞中的 FXR 蛋白水平，1 h 时即可检测到蛋白水平升高，且该升高趋势持续至 8 h[1]。
FXR DUBTAC IN-1 通过在 HepG2 细胞中促进 FXR 蛋白的去泛素化来稳定该蛋白，这一点可由处理后 FXR 多聚泛素化水平降低、FXR 蛋白水平升高的结果证实[1]。
FXR DUBTAC IN-1 可与纯化的 FXR 蛋白结合，通过表面等离子体共振法测得其解离常数 (Kd) 为 2.12 × 10-5 M[1]。
FXR DUBTAC IN-1 的 FXR 蛋白稳定作用在 HepG2 细胞中依赖于 OTUB1，因为敲低 OTUB1 可消除 FXR DUBTAC IN-1 诱导的 FXR 稳定化[1]。
FXR DUBTAC IN-1 (2 μM; up to 120 min) 在小鼠和大鼠肝微粒体中表现出良好的代谢稳定性，两种物种的半衰期均超过 120 min[1]。

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

FXR DUBTAC IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 1 μM, 10 μM, 50 μM
Incubation Time: 24 h (1 μM, 10 μM); no time specified (50 μM)
Result: Significantly increased FXR protein expression at 1 μM and further increased expression at 10 μM.
Maintained 70.71% cell viability at 50 μM.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 1 μM
Incubation Time: 1 h, 2 h, 4 h, 8 h
Result: Induced stabilization of FXR protein in a time-dependent manner, with FXR protein levels beginning to increase at 1 h after incubation.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-t CL
Rat[1] 2.5 mg/kg i.p. 11.00 h 1.50 h 18.84 ng/mL 82.53 ng·h/mL 419.78 mL/min/kg
Rat[1] 5 mg/kg i.p. 4.00 h 2.00 h 28.77 ng/mL 206.21 ng·h/mL 6.45 mL/min/kg
体内研究
(In Vivo)

FXR DUBTAC IN-1 (compound D11) (腹腔注射；每日 1 次，连续 5 天，剂量 1-2.5 mg/kg) 可稳定肝脏 FXR 蛋白，对 ANIT 诱导的胆汁淤积发挥强效、剂量依赖性的肝保护作用，在等效或更低剂量下，其疗效与 OCA 相当或更优[1]。
FXR DUBTAC IN-1 (腹腔注射，每日 1 次，连续 3 天，剂量 1-2.5 mg/kg) 以 OTUB1 依赖的方式减轻胆汁淤积性肝损伤，因为 OTUB1 敲低可完全消除其肝保护作用[1]。

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

Animal Model: C57BL/6J (male, 6 weeks old, 20 g, ANIT-induced cholestasis)[1]
Dosage: 1 mg/kg; 2.5 mg/kg
Administration: i.p.; daily; 5 days
Result: Significantly increased hepatic FXR protein levels in ANIT-induced cholestatic mice.
Caused significant, dose-dependent reductions in serum ALT, AST, ALP, and TBA levels.
Showed efficacy comparable to obeticholic acid (OCA) at 2.5 mg/kg at 1 mg/kg, and superior efficacy over OCA in reducing transaminases.
Improved liver histology as shown by hematoxylin-eosin (H&E) staining.
Animal Model: C57BL/6J (male, 6 weeks old, OTUB1 knockdown via AAV8-shRNA, ANIT-induced cholestasis)[1]
Dosage: 1 mg/kg; 2.5 mg/kg
Administration: i.p.; daily; 3 days
Result: Reversed ANIT-induced downregulation of hepatic FXR protein, significantly reduced elevated serum ALT, AST, ALP, and TBA levels, and improved liver histology in control shRNA-injected mice.
Failed to restore hepatic FXR protein levels, reduce serum cholestasis markers, or improve liver histology in OTUB1-knockdown mice.
分子量

751.01

Formula

C43H66N4O7
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

FXR DUBTAC IN-1 相关分类

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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.

Keywords:

FXR DUBTAC IN-13081876-96-9FXR DUBTAC IN1FXR DUBTAC IN 1DUBTACsDeubiquitinaseDeubiquitinase-targeting chimerasDUBsdeubiquitinaseubiquitin-proteasome systemfarnesoid X receptorα-naphthylisothiocyanate-induced cholestasisrat liver microsomesOTUB1HepG2 cellscholestatic liver injurypolyubiquitinationmiceInhibitorinhibitorinhibit

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