MZ-1

Catalog No.S8889 Batch:S888901

Technical Data

Formula	C₄₉H₆₀ClN₉O₈S₂
Molecular Weight	1002.64	CAS No.	1797406-69-9
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (99.73 mM)
		Ethanol	100 mg/mL (99.73 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

MZ-1 is a PROTAC degrader of bromodomain-containing protein 4 (BRD4). MZ-1 binds to the Brd bromodomain with Kd of 62 nM, 60 nM, 21 nM, 13 nM, 39 nM and 15 nM for Brd2^BD1, Brd2^BD2, Brd3^BD1, Brd3^BD2, Brd4^BD1 and Brd4^BD2.

Targets

Brd3(BD2) ^[1] (Cell-free assay)	Brd4(BD2) ^[1] (Cell-free assay)	Brd3(BD1) ^[1] (Cell-free assay)	Brd4(BD1) ^[1] (Cell-free assay)	Brd2(BD2) ^[1] (Cell-free assay)	View More
13 nM(Kd)	15 nM(Kd)	21 nM(Kd)	39 nM(Kd)	60 nM(Kd)	View More

In vitro

MZ-1 induces apoptosis of ovarian cancer cells and inhibits periostin-mediated ovarian cancer cell migration and invasion in vitro. MZ-1 specifically and efficiently inhibits the colony formation of periostin cells in soft agar, which clearly indicates a proproliferation role of periostin.^[2]

In vivo

Our in vivo studies shows significant growth inhibition by MZ-1 on both subcutaneous and intraperitoneal (i.p.) tumors derived from the periostin-expressing ovarian cancer cell line A2780. In addition, MZ-1 treatment leads to a reduction of the metastatic potential of these A2780 i.p. tumors. The in vivo antitumor effects of MZ-1 are linked to its specific inhibition of anchorage-independent growth and survival of periostin-expressing cells, as well as its neutralizing effects on periostin-induced cancer cell migration and invasion.^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines A2780, OAW-42, SKOV-3, TOV-112D, ES2, SP2/0 cell line Concentrations 20 μM Incubation Time 2 and 4 days Method In vitro apoptosis assay: Cells are grown in 24-well plates in serum-free medium (SFM) plus 1% BSA overnight to reach 50% to 60% confluency. A portion of 20 mg/mL of MZ-1 or control antibody is added into the wells. Cell apoptosis is analyzed 2 and 4 days later by using Annexin V-FITC Apoptosis Detection Kit. The cell flow cytometry is carried on Cell LabQuanta SC.
Animal Study:^{^[2]}	Animal Models Female SCID beige mice (6-8 weeks old) with A2780/TOV-112D xenografts Dosages 20 mg/kg Administration IH/SC, IP

Cell Assay:^{^[2]}

Cell lines
A2780, OAW-42, SKOV-3, TOV-112D, ES2, SP2/0 cell line
Concentrations
20 μM
Incubation Time
2 and 4 days
Method
In vitro apoptosis assay: Cells are grown in 24-well plates in serum-free medium (SFM) plus 1% BSA overnight to reach 50% to 60% confluency. A portion of 20 mg/mL of MZ-1 or control antibody is added into the wells. Cell apoptosis is analyzed 2 and 4 days later by using Annexin V-FITC Apoptosis Detection Kit. The cell flow cytometry is carried on Cell LabQuanta SC.

Animal Study:^{^[2]}

Animal Models
Female SCID beige mice (6-8 weeks old) with A2780/TOV-112D xenografts
Dosages
20 mg/kg
Administration
IH/SC, IP

References

Selleck's MZ-1 has been cited by 3 publications

Screening of an epigenetic compound library identifies BRD4 as a potential antiviral target for hepatitis B virus covalently closed circular DNA transcription [ Antiviral Res, 2023, 211:105552]	PubMed: 36737008
Dual mechanism: Epigenetic inhibitor apabetalone reduces SARS-CoV-2 Delta and Omicron variant spike binding and attenuates SARS-CoV-2 RNA induced inflammation [ Int Immunopharmacol, 2023, 117:109929]	PubMed: 36857935
Genomic Mapping of Splicing-Related Genes Identify Amplifications in LSM1, CLNS1A, and ILF2 in Luminal Breast Cancer [ Cancers (Basel), 2021, 13(16)4118]	PubMed: 34439272

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.