Cat. No.: HY-152147

SZUH280

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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.

For research use only. We do not sell to patients.

Purity: 99.38%
CAS No.: 2770263-77-7
Formula: C₃₆H₃₄N₈O₈
Molecular Weight:706.70

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

SZUH280 Chemical Structure

CAS No.: 2770263-77-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

HDAC8

0.58 μM (DC₅₀)

All PROTACs Isoforms :

All HDAC Isoforms :

All DNA/RNA Synthesis Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	9.55 μM Compound: D10	Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay	[PMID: 37607440]
A549	IC₅₀	6.04 μM Compound: 16e	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs under irradiation by CCK-8 method Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs under irradiation by CCK-8 method	[PMID: 36516047]
A549	IC₅₀	9.55 μM Compound: 16e	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 method Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 method	[PMID: 36516047]

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.

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.

Chemical Information

CAS No. 2770263-77-7
Appearance Solid
Molecular Weight 706.70
Formula C₃₆H₃₄N₈O₈
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4150 mL

7.0751 mL

14.1503 mL

5 mM

0.2830 mL

1.4150 mL

2.8301 mL

10 mM

0.1415 mL

0.7075 mL

1.4150 mL

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.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Huang J, et al. Structure-Based Discovery of Selective Histone Deacetylase 8 Degraders with Potent Anticancer Activity. J Med Chem. 2022 Dec 14. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

All PROTACs Isoforms

All HDAC Isoforms

All DNA/RNA Synthesis Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

SZUH280

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

All PROTACs Isoforms

All HDAC Isoforms

All DNA/RNA Synthesis Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

SZUH280 Related Classifications

HY-152147 Related Classifications