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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Based on 1 publication(s) in Google Scholar

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.
Appearance

Solid

Color

Light yellow to yellow

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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 116.67 mg/mL (165.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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SZUH280 Related Classifications

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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