MZ-1

For research use only.

Catalog No.S8889

MZ-1 Chemical Structure

CAS No. 1797406-69-9

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 Brd2BD1, Brd2BD2, Brd3BD1, Brd3BD2, Brd4BD1 and Brd4BD2.

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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 Brd2BD1, Brd2BD2, Brd3BD1, Brd3BD2, Brd4BD1 and Brd4BD2.
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)
13 nM(Kd) 15 nM(Kd) 21 nM(Kd) 39 nM(Kd) 60 nM(Kd)
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

Cell Research:

[2]

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  • 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.


    (Only for Reference)
Animal Research:

[2]

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

Solubility (25°C)

In vitro DMSO 100 mg/mL (99.73 mM)
Ethanol 100 mg/mL (99.73 mM)
Water 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.

Chemical Information

Molecular Weight 1002.64
Formula

C49H60ClN9O8S2

CAS No. 1797406-69-9
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NCCOCCOCCOCC(=O)NC(C(=O)N4CC(CC4C(=O)NCC5=CC=C(C=C5)C6=C(N=CS6)C)O)C(C)(C)C)C7=CC=C(C=C7)Cl)C

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID