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]. |
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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. |
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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. |
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| 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. |
