1. PROTAC Epigenetics Cell Cycle/DNA Damage Apoptosis
  2. PROTACs HDAC Apoptosis DNA/RNA Synthesis
  3. 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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Customer Review

  • 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.

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
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 116.67 mg/mL (165.09 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4150 mL 7.0751 mL 14.1503 mL
5 mM 0.2830 mL 1.4150 mL 2.8301 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4150 mL 7.0751 mL 14.1503 mL 35.3757 mL
5 mM 0.2830 mL 1.4150 mL 2.8301 mL 7.0751 mL
10 mM 0.1415 mL 0.7075 mL 1.4150 mL 3.5376 mL
15 mM 0.0943 mL 0.4717 mL 0.9434 mL 2.3584 mL
20 mM 0.0708 mL 0.3538 mL 0.7075 mL 1.7688 mL
25 mM 0.0566 mL 0.2830 mL 0.5660 mL 1.4150 mL
30 mM 0.0472 mL 0.2358 mL 0.4717 mL 1.1792 mL
40 mM 0.0354 mL 0.1769 mL 0.3538 mL 0.8844 mL
50 mM 0.0283 mL 0.1415 mL 0.2830 mL 0.7075 mL
60 mM 0.0236 mL 0.1179 mL 0.2358 mL 0.5896 mL
80 mM 0.0177 mL 0.0884 mL 0.1769 mL 0.4422 mL
100 mM 0.0142 mL 0.0708 mL 0.1415 mL 0.3538 mL
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.

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产品名称:
SZUH280
目录号:
HY-152147
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