2. PROTAC Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. PROTACs HDAC Apoptosis DNA/RNA Synthesis
  4. SZUH280

SZUH280 是一种有效的、选择性的 PROTAC HDAC8 降解剂，在 A549 细胞中的 DC50 为 0.58 μM。SZUH280 诱导癌细胞凋亡 (apoptosis)。SZUH280 在癌细胞中阻碍 DNA 损伤修复，促进细胞放射致敏。

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SZUH280 Chemical Structure

SZUH280 Chemical Structure

CAS No. : 2770263-77-7

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SZUH280 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

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SZUH280 is a potent and selective PROTAC HDAC8 degrader with a DC50 of 0.58 μM in A549 cells. SZUH280 induces cancer cell apoptosis. SZUH280 hampers DNA damage repair in cancer cells, promoting cellular radiosensitization[1].

IC50 & Target[1]

HDAC8

0.58 μM (DC50)

体外研究
(In Vitro)

SZUH280 (5 μM; 20 h) 降解 HDAC8 由 CRBN E3 泛素连接酶介导[1]。
SZUH280 (0.1-10 μM; 20 h) 可调节致癌蛋白表达，抑制癌症转移，可能提高各种类型癌症的化疗疗效[1]。
SZUH280 (0-20 μM; 72 h) 以浓度依赖方式抑制 A549 细胞增殖，且与放射联合使用时，其抗增殖作用更强[1]。
SZUH280 (0-20 μM; 72 h) 诱导 A549 细胞凋亡，阻滞细胞周期于 G2/M 期[1]。
SZUH280 (5 μM; 24 h) 与辐射联合使用时，阻碍癌细胞 DNA 损伤修复[1]。

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

SZUH280 相关抗体:

Western Blot Analysis[1]

Cell Line: A549, HCT116, HeLa and MDA-MB-231 cells
Concentration: 0.1, 0.3, 1, 3 and 10 μM
Incubation Time: 20 h
Result: Efficiently induced HDAC8 degradation in a concentration-dependent manner in A549, HCT116 and HeLa cells. Reduced the IKZF1 protein levels to a lesser extent at 10 μM in A549 cells. Decreased PGM1 expression during glucose deprivation conditions in A549 cells. Decreased SMAD3 and HDAC8 protein levels in MDA-MB-231 cells.

Cell Proliferation Assay[1]

Cell Line: A549 cells
Concentration: 2.5, 5, 10 and 20 μM
Incubation Time: 72 h
Result: Effectively inhibited cell proliferation in a concentration-dependent manner with an IC50 of 9.55 μM. Co-treatment with irradiation exhibited an even stronger antiproliferative effect (with an IC50 value of about 6.04 μM).

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 1.25, 2.5, 5, 10 and 20 μM
Incubation Time: 72 h
Result: Effectively induced apoptosis in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 1.25, 2.5, 5, 10 and 20 μM
Incubation Time: 72 h
Result: Induced cell cycle arrest at the G2/M phase.
体内研究
(In Vivo)

SZUH280 (5 mg/kg; i.p.; every 5 days for 6 weeks) 在 A549 裸鼠模型中显示抗肿瘤活性[1]。

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

Animal Model: NOD/SCID mice (severe combined immunodeficient mice), A549 model[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection, every 5 days for 6 weeks
Result: Exhibited a significantly greater anti-lung cancer activity in vivo than the control group. When in combination with 3 Gy irradiation, achieved a much stronger antitumor activity.
分子量

706.70

Formula

C36H34N8O8
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

SZUH280 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

SZUH2802770263-77-7SZUH 280SZUH-280PROTACsHDACApoptosisDNA/RNA SynthesisHistone deacetylasesA549HCT116HeLaradiosensitizationInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-152147
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