2. PROTAC Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Apoptosis
  3. PROTACs RAR/RXR Androgen Receptor Apoptosis Caspase MDM-2/p53
  4. WCF-598

WCF-598 是一种 RXRγ (Kd: 234.2 nM) 和 AR-V7 PROTAC 降解剂。WCF-598 通过泛素-蛋白酶体通路诱导 RXRγ 降解，可直接结合 RXRγ。WCF-598 可间接诱导 AR-V7 降解，破坏 RXRγ-AR-V7 复合物的稳定性，下调 AR-V7 水平，并抑制 AR-V7 下游靶基因的转录。WCF-598 可诱导肿瘤细胞凋亡 (apoptosis)，抑制细胞增殖，激活 p53 信号通路，并抑制细胞周期进程。WCF-598 可用于前列腺癌的研究。(粉色：靶蛋白配体 HY-182352；蓝色：E3 连接酶配体 HY-138793)。

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WCF-598

WCF-598 Chemical Structure

CAS No. : 3059574-58-9

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WCF-598 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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RXRα RXRβ RXRγ

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WCF-598 is a RXRγ (Kd: 234.2 nM) and AR-V7 PROTAC degrader. WCF-598 induces RXRγ degradation via the ubiquitin-proteasome pathway and binds directly to RXRγ. WCF-598 indirectly induces AR-V7 degradation, impairs the stability of the RXRγ-AR-V7 complex, downregulates AR-V7 levels, and inhibits the transcription of downstream target genes of AR-V7. WCF-598 induces tumor cell apoptosis, inhibits cell proliferation, activates the p53 signaling pathway, and suppresses cell cycle progression. WCF-598 can be used for the research of prostate cancer. (Pink: target protein ligand HY-182352; Blue: E3 ligase ligand HY-138793)[1].

IC50 & Target[1]

RXRγ

 

体外研究
(In Vitro)

WCF-598 (96 h) 可强效抑制 22Rv1 细胞的活力，其 IC50 为 13.56 nM，对 VCaP-CRPC 细胞的 IC50 为 88.46 nM[1]。
WCF-598 (6.25-6400 nM; 48 h) 可剂量依赖性降解 22Rv1 细胞和 VCaP-CRPC 细胞中的 RXRγ 蛋白[1]。
WCF-598 (6.25-6400 nM; 48 h) 可在 22Rv1 细胞中呈剂量依赖性降解 AR-V7 蛋白，处理 48 h 后的 DC50 为 122.0 nM[1]。
WCF-598 (100-400 nM; 14 days) 可强效且呈浓度依赖性地抑制 22Rv1 细胞的集落形成[1]。
WCF-598 (100-400 nM; 72 h) 可浓度依赖性地诱导 22Rv1 细胞发生细胞凋亡，其作用可通过剪切型 PARP、caspase-7 水平升高及 Caspase-3/7 活性增强得以体现[1]。
WCF-598 (100-400 nM; 48 h) 以浓度依赖性方式激活 p53 相关通路并抑制 22Rv1 细胞周期相关通路[1]。

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

WCF-598 相关抗体:

Western Blot Analysis[1]

Cell Line: 22Rv1, VCaP-CRPC
Concentration: 6.25, 12.5, 25, 50, 100, 200, 400, 800, 1600, 3200, 6400 nM
Incubation Time: 48 h
Result: Induced dose-dependent degradation of RXRγ in both cell lines, with DC50 values of 24.82 nM (22Rv1, maximal degradation 92.79%) and 27.15 nM (VCaP-CRPC, maximal degradation 82.01%).

Apoptosis Analysis[1]

Cell Line: 22Rv1
Concentration: 100, 200, 400 nM
Incubation Time: 72 h
Result: Induced concentration-dependent apoptosis in 22Rv1 cells, demonstrated by increased levels of cleaved-PARP and caspase-7, and significantly elevated Caspase-3/7 activity at all tested concentrations.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-t MRT0-t F Vz CL
Rat[1] 3.0 mg/kg i.v. 3.85 h 0.08 h 39187.77 ng/mL 17400.36 ng·h/mL 0.86 h / 0.98 L/kg 2.91 mL/min/kg
Rat[1] 10.0 mg/kg p.o. 2.43 h 0.83 h 117.71 ng/mL 243.45 ng·h/mL 2.09 h 0.42 % / /
Rat[1] 5.0 mg/kg i.p. 7.69 h 5.33 h 743.64 ng/mL 6649.49 ng·h/mL 8.66 h 22.93 % / /
体内研究
(In Vivo)

WCF-598 (10-20 mg/kg；腹腔注射；每日给药；17 天) 可剂量依赖性地抑制 NOD-SCID 小鼠体内 22Rv1 去势抵抗性前列腺癌 (CRPC) 异种移植瘤的生长[1]。

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

Animal Model: NOD-SCID (male, 4 weeks old, injected subcutaneously with 22Rv1 CRPC cells)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; daily; 17 days
Result: Achieved a tumor growth inhibition (TGI) value of 45.46% at 10 mg/kg.
Achieved a tumor growth inhibition (TGI) value of 61.18% at 20 mg/kg.
Significantly downregulated RXRγ protein levels in tumor tissues at both doses.
Induced degradation of androgen receptor (AR) and androgen receptor splice variant 7 (AR-V7) proteins in tumor tissues at both doses.
Caused no significant changes in mouse body weight during treatment.
Resulted in normal morphology and function of major organs (heart, liver, spleen, lung, kidney) per histopathological analysis.
分子量

894.11

Formula

C54H63N5O7
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

WCF-598 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:

WCF-5983059574-58-9WCF598WCF 598PROTACsRAR/RXRAndrogen ReceptorApoptosisCaspaseMDM-2/p53Retinoic acid receptorsRetinoid X receptorscastration-resistant prostate cancerp53 signaling pathwayCRPC cellsubiquitin-proteasome pathwayapoptosisRXRγAR-V7VCaP-CRPC cellsnuclear receptors22Rv1 cellsInhibitorinhibitorinhibit

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目录号：
HY-182331
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