2. PROTAC Vitamin D Related/Nuclear Receptor Apoptosis
  3. Molecular Glues Androgen Receptor Caspase Apoptosis
  4. AR Degrader-3

AR Degrader-3 一种具有口服活性的分子胶 (molecular glue)，靶向 AR/ARV7, 通过泛素-蛋白酶体途径 (UPP) 诱导 AR 和 ARV7 降解。AR Degrader-3 可直接与 AR 的配体结合域 (LBD) 和 N 端结构域 (NTD) 相互作。AR Degrader-3 能有效抑制野生型 AR (AR-WT)、AR 突变体和 ARV7 的转录活性。AR Degrader-3 可下调下游 AR 靶基因的 mRNA 和蛋白水平，从而克服由 ARV7 和 AR 点突变介导的抗雄激素耐药性。AR Degrader-3 可诱导 Enzalutamide (HY-70002) (ENZa) 耐药细胞凋亡 (apoptosis)，并增加裂解型 caspase-3 蛋白的水平。AR Degrader-3 可用于去势抵抗性前列腺癌 (CRPC) 的研究。

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AR Degrader-3

AR Degrader-3 Chemical Structure

CAS No. : 1182011-65-9

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AR Degrader-3 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

AR Degrader-3 is an orally active molecular glue that targets AR/ARV7 and induces the degradation of AR and ARV7 through the ubiquitin-proteasome pathway (UPP). AR Degrader-3 directly interacts with the ligand-binding domain (LBD) and the N-terminal domain (NTD) of AR. AR Degrader-3 effectively suppresses the transcriptional activity of wild-type AR (AR-WT), AR mutants, and ARV7. AR Degrader-3 downregulates the mRNA and protein levels of downstream AR target genes, thereby overcoming antiandrogen resistance mediated by ARV7 and AR point mutations. AR Degrader-3 induces apoptosis in Enzalutamide (HY-70002) (ENZa)-resistant cells and increases cleaved caspase-3 protein levels. AR Degrader-3 can be used for the study of castration-resistant prostate cancer (CRPC)[1].
IC50 & Target

Caspase-3

 

体外研究
(In Vitro)

AR Degrader-3 (Compound A6) (0.2-5 μM，24 小时) 通过剂量依赖性地抑制 PC-3 和 C4-2 细胞中外源性和内源性 AR 的表达，从而广泛抑制 AR 的转录活性；此外，它还显著抑制了 Enzalutamide 耐药的 22Rv1 细胞中的内源性 AR 和 ARV7 的表达，并抑制了 PC-3 细胞中 AR 突变体 (W741L、T877A、F876L) 的转录活性[1]。
AR Degrader-3 (0.078-10 μM，0-36 小时) 以剂量依赖性的方式抑制 22Rv1 细胞中 ARV7 的蛋白水平 (DC50 = 0.24 μM) ，显著下调 C4-2 细胞中 AR 的蛋白水平 (DC50 = 0.18 μM) ，并以时间依赖性的方式下调 ARV7 的蛋白水平[1]。
AR Degrader-3 能有效抑制 LNCaP 细胞中的 AR 和 ARV7，其机制是通过直接结合 AR-LBD (IC50 = 105.4 nM) 和 AR-AF1 (KD = 23.0 μM)[1]。
AR Degrader-3 (1-5 μM，4-8 小时) 通过泛素-蛋白酶体途径 (UPP) 降解 AR 和 ARV7，体现在 C4-2 和 22Rv1 细胞中，AR Degrader-3 分别剂量依赖性地降低 AR 和 ARV7 的蛋白水平 (而非 mRNA 水平) ；环己酰亚胺处理可加速 AR 和 ARV7 的降解；MG132 可拮抗 AR Degrader-3 的蛋白水平降低作用；以及 AR Degrader-3 显著诱导 AR 的泛素化[1]。
AR Degrader-3 (72 小时) 抑制 C4-2 细胞 (IC50 = 0.59 μM) 和 22Rv1 细胞 (IC50 = 1.4 μM) 的增殖，但对 DU145 细胞 (IC50 > 50 μM) 和 PC-3 细胞 (IC50 = 48.6 μM) 的影响甚微[1]。
AR Degrader-3 (0.2-5 μM，8-24 小时) 以剂量依赖的方式阻断 R1881 诱导的 PSA 蛋白表达，并降低 22Rv1 细胞中 PSA 和 PMEPA1 的 mRNA 水平[1]。
AR Degrader-3 (1-2 μM，14 天) 选择性地减少 22Rv1 细胞的克隆形成数量，但对 AR 阴性的 PC-3 细胞的克隆形成数量没有影响，并促进 22Rv1 细胞的凋亡[1]。

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

AR Degrader-3 相关抗体:

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Significantly downregulated the level of ARV7.

Western Blot Analysis[1]

Cell Line: 22Rv1 cells, C4-2 cells
Concentration: 0.078 μM, 0.156 μM, 0.31 μM, 0.62 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Dose-dependently suppressed ARV7 (DC50 = 0.24 μM) protein level in 22Rv1 cells, down-regulated AR (DC50 = 0.18 μM) protein level in C4-2 cells.

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 0.2 μM, 1 μM, 5 μM
Incubation Time: 24 h
Result: Blocked R1881-induced PSA protein expression in a dose-dependent manner in 22Rv1 cells.

RT-PCR[1]

Cell Line: 22Rv1 cells
Concentration: 0.2 μM, 1 μM, 5 μM
Incubation Time: 8 h
Result: Reduced the mRNA level of PSA in 22Rv1 cells.

RT-PCR[1]

Cell Line: 22Rv1 cells
Concentration: 0.2 μM, 1 μM, 5 μM
Incubation Time: 24 h
Result: Reduced the mRNA level of PMEPA1 in 22Rv1 cells.

Cell Proliferation Assay[1]

Cell Line: 22Rv1 cells, PC-3 cells
Concentration: 1 μM, 2 μM
Incubation Time: 14 days
Result: Decreased 22Rv1 cells colony numbers but showed no influence on AR-negative PC-3 cells colony numbers.
体内研究
(In Vivo)

AR Degrader-3 (Compound A6) (15-30 mg/kg，口服，每日一次，持续 14 天) 可有效抑制 22Rv1 细胞荷瘤小鼠体内 CRPC 肿瘤的生长，且未观察到明显的毒性[1]。

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

Animal Model: Male BALB/c nude mice (5-week-old) were subcutaneously inoculated with 5 × 106 22Rv1 cells[1].
Dosage: 15 mg/kg, 30 mg/kg
Administration: P.o., once daily for 14 days
Result: Suppressed 22Rv1 tumor progression.
Showed no change in body weight.
Significantly decreased AR levels in the tumor tissues.
分子量

435.50

Formula

C23H21N3O4S
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

AR Degrader-3 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:

AR Degrader-31182011-65-9AR Degrader3AR Degrader 3Molecular GluesAndrogen ReceptorCaspaseApoptosisAndrogen receptorAntiandrogenCastration-resistant prostate cancerDegraderDrug resistanceInhibitorinhibitorinhibit

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