SZUH280

Cat. No.: HY-152147: FAQs
Data Sheet Handling Instructions

Molarity Calculator

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.

SZUH280 Chemical Structure

CAS No. : 2770263-77-7

Size	Price	Stock
5 mg	USD 422	Ask For Quote & Lead Time
10 mg	USD 705	Ask For Quote & Lead Time
25 mg	USD 1484	Ask For Quote & Lead Time
50 mg	USD 2375	Ask For Quote & Lead Time
100 mg	USD 3800	Ask For Quote & Lead Time

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All PROTACs Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All HDAC Isoform Specific Products:

View All Isoforms

HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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.

2770263-77-7

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

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]

SZUH280 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks