Home Epigenetics Epigenetic Reader Domain modulator - PROTAC modulator MZ-1 For research use only.

MZ-1

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.

MZ-1 Chemical Structure

MZ-1 Chemical Structure

CAS: 1797406-69-9

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

Purity & Quality Control

Batch: Purity: 99.58%
99.58

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Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

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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)		 Click to View More Targets
13 nM(Kd) 15 nM(Kd) 21 nM(Kd) 39 nM(Kd) 60 nM(Kd)
In vitro
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Female SCID beige mice (6-8 weeks old) with A2780/TOV-112D xenografts
Dosages 20 mg/kg
Administration IH/SC, IP

Chemical Information & Solubility

Molecular Weight 1002.64 Formula

C49H60ClN9O8S2
CAS No. 1797406-69-9 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (99.73 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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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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