2. PROTAC Cell Cycle/DNA Damage Apoptosis Immunology/Inflammation
  3. PROTACs RAD51 DNA/RNA Synthesis Apoptosis IKZF Family
  4. SZU305

SZU305 是一种 RAD51 PROTAC 降解剂，其在 SK-HEP-1 和 Huh-7 中的 DC50 分别为 307.45 和 84.19 nM。SZU305 抑制 DNA 损伤修复，诱导细胞周期阻滞和细胞凋亡 (apoptosis)。SZU305 在高浓度下可适度降低 IKZF1 和 IKZF3 的蛋白水平。SZU305 可用于肝细胞癌的相关研究。
(粉色: RAD51 配体 (HY-167881)；蓝色: Cereblon 配体 (HY-W087383)；黑色: 连接子)。

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SZU305

SZU305 Chemical Structure

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SZU305 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 IKZF Family 亚型特异性产品:

查看所有亚型
IKZF1 IKZF2 IKZF3 IKZF4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SZU305 is a RAD51 PROTAC degrader, with DC50 values of 307.45 nM and 84.19 nM in SK-HEP-1 and Huh-7 cells, respectively. SZU305 inhibits DNA damage repair, induces cell cycle arrest and apoptosis. SZU305 moderately reduces the protein levels of IKZF1 and IKZF3 at high concentrations. SZU305 can be used in studies related to hepatocellular carcinoma[1]. (Pink: RAD51 ligand (HY-167881); Blue: Cereblon ligand (HY-W087383); Black: linker).

IC50 & Target[1]

Cereblon

 

IKZF1

 

IKZF3

 

体外研究
(In Vitro)

SZU305 (0.3-3 μM; 48 h) 可在 3 μM 处理 48 h 后，强效诱导人肝癌细胞 SK-HEP-1 中的 RAD51 近乎完全降解[1]。
SZU305 (3 μM; 48 h) 移除会导致人肝癌细胞 SK-HEP-1 中的 RAD51 蛋白水平在 24 h 内逐渐恢复，表明 RAD51 的周转速率相对较慢[1]。
SZU305 (3 μM; 48 h) 可通过 CRBN 及蛋白酶体依赖的机制诱导人肝癌细胞系 SK-HEP-1 中的 RAD51 降解，且该降解过程依赖于类泛素化修饰以及与 RAD51 催化位点的竞争性结合[1]。
SZU305 (0.5-10 μM; 72 h) 在处理 72 h 后，对人肝癌细胞 SK-HEP-1 具有浓度依赖性的抗增殖活性[1]。
SZU305 (1.25-10 μM; 12-14 days) 可强效抑制人肝癌细胞 SK-HEP-1 的集落形成[1]。
SZU305 (5-10 μM; 72 h) 可在 5 μM 和 10 μM 浓度下处理 SK-HEP-1 人肝癌细胞 72 h 后，诱导细胞发生剂量依赖性的 G2/M 期细胞周期阻滞[1]。
SZU305 (5-10 μM; 72 h) 处理 72 h 后可在人肝癌细胞 SK-HEP-1 中诱导剂量依赖性细胞凋亡[1]。
SZU305 (3 μM; 48 h) 可在 SK-HEP-1 人肝癌细胞中选择性降解 RAD51 蛋白，而在 3 μM 处理 48 h 后不会显著改变其 mRNA 水平，同时可调控参与 DNA 损伤修复、细胞凋亡和应激反应的基因与蛋白的表达[1]。
SZU305 (3 μM; 48 h) 可增强 SK-HEP-1 人肝癌细胞的 DNA 损伤[1]。
SZU305 (48 h) 处理 DR-U2OS 报告细胞 48 h 后会损害其同源重组修复效率，但对 EJ5-U2OS 报告细胞中的非同源末端连接无显著影响[1]。
SZU305 在与 3 Gy IR 联合作用时会增加人肝癌细胞系 SK-HEP-1 的染色体断裂，提示 DNA 损伤修复功能受损[1]。
SZU305 可损伤人肝癌细胞系 SK-HEP-1 中 γ-H2AX 灶的形成，且与 VP16、CPT、sorafenib 或 IR 联用时该作用会增强，提示其可破坏 DNA 损伤应答[1]。

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

SZU305 相关抗体:

Western Blot Analysis[1]

Cell Line: SK-HEP-1 human liver cancer cells
Concentration: 0.3 μM; 3 μM
Incubation Time: 48 h
Result: Induced ~99% RAD51 degradation at 3 μM after 48 h.

Western Blot Analysis[1]

Cell Line: SK-HEP-1 human liver cancer cells
Concentration: 3 μM
Incubation Time: 48 h (15b treatment); 0, 4, 8, 12, 24 h (drug-free recovery)
Result: Allowed RAD51 protein expression to gradually recover within 24 h after removal.

Western Blot Analysis[1]

Cell Line: SK-HEP-1 human liver cancer cells
Concentration: 3 μM (15b treatment); MG132, MLN4924, pomalidomide, RI-1, 5a (pretreatment); siCRBN (pretreatment)
Incubation Time: 48 h (15b treatment); 2 h (MG132, MLN4924, pomalidomide, RI-1, 5a pretreatment); 48 h (siCRBN pretreatment)
Result: Had RAD51 degradation completely abolished by co-incubation with MG132.
Showed RAD51 degradation prevented or diminished by MLN4924, pomalidomide, RI-1, 5a, and siCRBN.

Cell Viability Assay[1]

Cell Line: SK-HEP-1 human liver cancer cells
Concentration: 0.5, 1, 2.5, 5, 10 μM
Incubation Time: 72 h
Result: Inhibited SK-HEP-1 cell proliferation in a concentration-dependent manner, with reduced cell viability observed at all tested concentrations.

Cell Proliferation Assay[1]

Cell Line: SK-HEP-1 human liver cancer cells
Concentration: 1.25, 2.5, 5 and 10 μM
Incubation Time: 12-14 days
Result: Suppressed colony formation more effectively than RI-1 at equivalent concentrations.

Cell Cycle Analysis[1]

Cell Line: SK-HEP-1 human liver cancer cells
Concentration: 5 μM; 10 μM
Incubation Time: 72 h
Result: Induced dose-dependent cell cycle arrest at the G2/M phase, with G1 phase population reduced from 80.15% (control) to 50.07% (5 μM) and 46.36% (10 μM), while G2/M phase population increased from 12.49% (control) to 34.63% (5 μM) and 38.42% (10 μM).

Apoptosis Analysis[1]

Cell Line: SK-HEP-1 human liver cancer cells
Concentration: 5 μM; 10 μM
Incubation Time: 72 h
Result: Induced dose-dependent apoptosis, with up to ~23% apoptotic cells observed at 10 μM.
体内研究
(In Vivo)

SZU305 (15 mg/kg; i.v..; 每隔一天一次，共 3 次) 在 Huh-7 肝癌异种移植小鼠模型中展现出强效的体内抗肿瘤活性且毒性较低[1]。

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

Animal Model: BALB/c nude (4-6 weeks old)[1]
Dosage: 15 mg/kg
Administration: i.v.; once every other day, 3 doses total
Result: Suppressed tumor growth with a T/C ratio of 75.6%.
Combined with sorafenib, achieved a T/C ratio of 16.7%.
Combined with 3 Gy irradiation, achieved a T/C ratio of 2.3%.
Caused no body weight loss, indicating low toxicity.
Induced RAD51 degradation in tumor tissue.
Reduced RAD51 and Ki67 expression in tumor tissue.
Elevated cleaved caspase-3 levels in tumor tissue, with greater effects seen in combination with sorafenib or irradiation.
分子量

717.96

Formula

C32H28Cl3FN6O6
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

SZU305 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:

SZU305SZU 305SZU-305PROTACsRAD51DNA/RNA SynthesisApoptosisIKZF FamilyIkaros zinc finger protein familyhepatocellular carcinomaSK-HEP-1Huh-7proteasomeliver cancer cellshomologous recombination DNA repairCRBNIKZF3IKZF1Inhibitorinhibitorinhibit

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