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

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.

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SZUH280 Chemical Structure

SZUH280 Chemical Structure

CAS No. : 2770263-77-7

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SZUH280 Related Antibodies

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Description

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)

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].

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

SZUH280 Related Antibodies

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.
In Vivo

SZUH280 (5 mg/kg; i.p.; every 5 days for 6 weeks) shows antitumor activity in an A549 nude mouse model[1].

MedChemExpress (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.
Molecular Weight

706.70

Formula

C36H34N8O8
CAS No.
SMILES

O=C(C1=CC=C2C(N(C=C2)CC3=CC=C(C=C3)OCCOCCN4C=C(N=N4)CNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)=C1)NO
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SZUH280 Related Classifications

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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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