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SZUH280
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SZUH280图片
CAS NO:2770263-77-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

SZUH280 is a potent and selectivePROTACHDAC8degrader with aDC50of 0.58 μM in A549 cells. SZUH280 inducescancercellapoptosis. SZUH280 hampersDNA damagerepair incancercells, promoting cellular radiosensitization[1].

IC50& Target[1]

HDAC8

0.58 μM (DC50)

体外研究
(In Vitro)

HDAC8 degradation induced by SZUH280 (5 μM; 20 h) is mediated by the CRBN E3 ubiquitin ligase[1].
SZUH280 (0.1-10 μM; 20 h) can regulate the oncogenic protein expression and suppress cancer metastasis, potentially improving the efficacy of chemotherapy in various types of cancers[1].
SZUH280 (0-20 μM; 72 h) inhibits A549 cell proliferation in a concentration-dependent manner and shows stronger antiproliferative effect with irradiation[1].
SZUH280 (0-20 μM; 72 h) induces apoptosis and arrests cell cycle at G2/M phase in A549 cells[1].
SZUH280 (5 μM; 24 h) hampers DNA damage repair in cancer cells when in combination with irradiation[1].

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 IC50of 9.55 μM. Co-treatment with irradiation exhibited an even stronger antiproliferative effect (with an IC50value 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) shows antitumor activity in an A549 nude mouse model[1].

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

2770263-77-7

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.