2. PROTAC Metabolic Enzyme/Protease Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain E1/E2/E3 Enzyme Apoptosis
  4. PROTAC RNF4 degrader-1

PROTAC RNF4 degrader-1 是一种 PROTAC 类 RNF4 降解剂 (Kd = 64.5 nM)，可通过泛素-蛋白酶体系统降解 RNF4。PROTAC RNF4 degrader-1 可诱导 DNA 损伤、细胞凋亡 (apoptosis)，并在癌细胞中表现出抗增殖活性。PROTAC RNF4 degrader-1 在小鼠模型中表现出抗肿瘤活性，且无明显副作用。PROTAC RNF4 degrader-1 可用于肝细胞癌的研究。

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PROTAC RNF4 degrader-1

PROTAC RNF4 degrader-1 Chemical Structure

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PROTAC RNF4 degrader-1 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader (Kd = 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system. PROTAC RNF4 degrader-1 induces DNA damage, apoptosis, and exhibits antiproliferative activity in cancer cells. PROTAC RNF4 degrader-1 displays antitumor activity with no obvious side effects in mouse models. PROTAC RNF4 degrader-1 is applicable to the research of hepatocellular carcinoma[1].

IC50 & Target[1]

VHL

 

RNF4

64.5 nM (Kd)

体外研究
(In Vitro)

PROTAC RNF4 degrader-1 (Compound RD12) (0.2-20 μM; 72 h) 可强效抑制人肝癌细胞 HepG2 的增殖，其 IC50 为 0.48 μM[1]。
PROTAC RNF4 degrader-1 (0.1-10 μM; 6 h) 可在人肝癌细胞 HepG2 中诱导 RNF4 蛋白呈剂量依赖性降解[1]。
PROTAC RNF4 degrader-1 (0-20 μM; 6 h) 可在人肝癌 Huh7 细胞中诱导 RNF4 蛋白的剂量依赖性降解，其 DC50 为 4.16 μM[1]。
PROTAC RNF4 degrader-1 (5 μM; 6 h after 2 h pre-incubation with MG132) 介导的人肝癌细胞 HepG2 和 Huh7 中 RNF4 降解依赖于泛素-蛋白酶体系统，因为用蛋白酶体抑制剂 MG132 预处理可逆转 RNF4 的缺失[1]。
PROTAC RNF4 degrader-1 (0.1-10 μM; 6 h) 可在人肝癌细胞 HepG2 和 Huh7 中诱导剂量依赖性的 DNA 损伤，该效应通过 γH2AX 水平的升高得到验证[1]。
PROTAC RNF4 degrader-1 (0-20 μM; 6 h) 以剂量依赖方式在人肝癌 Huh7 细胞中上调 RNF4 底物蛋白 BRCA1 和 MDC1 的水平，该结果与 RNF4 降解的情况一致[1]。
PROTAC RNF4 degrader-1 (serial two-fold dilutions; 30 min at room temperature) 可直接与重组 RNF4 蛋白结合，通过 MST[1] 测得其 Kd 为 64.5 nM。
PROTAC RNF4 degrader-1 (10 μM; 6 h) 可在人肝癌 Huh7 细胞中选择性诱导 RNF4 降解，在鉴定出的 7483 种蛋白质中，仅 28 种出现显著下调[1]。
PROTAC RNF4 degrader-1 (5 μM; 48 h) 可诱导 52.1%的人肝癌 Huh7 细胞发生凋亡[1]。

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

PROTAC RNF4 degrader-1 相关抗体:

Cell Viability Assay[1]

Cell Line: HepG2 human hepatocellular carcinoma cells
Concentration: 0.2, 2, 20 μM
Incubation Time: 72 h
Result: Inhibited HepG2 cell proliferation with an IC50 of 0.48 ± 0.095 μM.

Western Blot Analysis[1]

Cell Line: HepG2 human hepatocellular carcinoma cells
Concentration: 0.1, 1.25, 2.5, 5, 10 μM
Incubation Time: 6 h
Result: Induced dose-dependent degradation of RNF4 protein, with reduced RNF4 levels observed at all tested concentrations relative to untreated cells.

Western Blot Analysis[1]

Cell Line: Huh7 human hepatocellular carcinoma cells
Concentration: 0.1, 1.25, 2.5, 5, 10 μM; 0, 0.625, 1.25, 2.5, 5, 10, 20 μM
Incubation Time: 6 h
Result: Induced dose-dependent degradation of RNF4 protein with a DC50 (degradation half-maximal concentration) of 4.16 ± 0.222 μM.

Western Blot Analysis[1]

Cell Line: HepG2 and Huh7 human hepatocellular carcinoma cells
Concentration: 5 μM
Incubation Time: 6 h (after 2 h pre-incubation with MG132)
Result: Mediated RNF4 degradation that was rescued by pre-treatment with MG132, confirming dependency on the ubiquitin-proteasome system.

Western Blot Analysis[1]

Cell Line: HepG2 and Huh7 human hepatocellular carcinoma cells
Concentration: 0.1, 1.25, 2.5, 5, 10 μM
Incubation Time: 6 h
Result: Induced dose-dependent increases in γH2AX levels (a marker of DNA double-strand breaks), with higher γH2AX expression observed at higher concentrations.

Western Blot Analysis[1]

Cell Line: Huh7 human hepatocellular carcinoma cells
Concentration: 0, 5, 10, 20 μM
Incubation Time: 6 h
Result: Induced dose-dependent increases in BRCA1 and MDC1 protein levels (known substrates of RNF4), corresponding to reduced RNF4 levels.

Apoptosis Analysis[1]

Cell Line: Huh7 human hepatocellular carcinoma cells
Concentration: 5 μM
Incubation Time: 48 h
Result: Induced apoptosis in 52.1% of Huh7 cells, as measured by Annexin V staining.
体内研究
(In Vivo)

PROTAC RNF4 degrader-1 (Compound RD12) (5-20 mg/kg；腹腔注射；每 2 天 1 次, 共 20 天) 可在 BALB/c 裸鼠中诱导显著的剂量依赖性肝癌肿瘤生长抑制，在 5 mg/kg 和 20 mg/kg 剂量下的抑制率分别为 58% 和 76%，且未产生可观察到的肝毒性或体重下降[1]。

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

Animal Model: BALB/c nude (6-week-old, female, subcutaneously implanted with Huh7 cells)[1]
Dosage: 5 mg/kg; 20 mg/kg
Administration: i.p.; once every two days; 20 days
Result: Achieved tumor growth inhibition rates of 58% at 5 mg/kg and 76% at 20 mg/kg compared to vehicle controls.
Induced significant degradation of RNF4 protein in tumor tissues at 5 mg/kg.
Caused no significant changes in mouse body weight.
Resulted in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels similar to healthy controls, indicating no liver toxicity.
分子量

866.46

Formula

C47H52ClN5O7S
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

PROTAC RNF4 degrader-1 相关分类

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Help & FAQs
  • 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:

PROTAC RNF4 degrader-1PROTACsEpigenetic Reader DomainE1/E2/E3 EnzymeApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseubiquitin-proteasome systemcancer cellsmouse modelDNA damageHepG2 human hepatocellular carcinoma cellsapoptosishepatocellular carcinomaHuh7 human hepatocellular carcinoma cellsBRCA1RNF4Inhibitorinhibitorinhibit

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