Chemical Name: (2S,4R)-1-((S)-2-(tert-butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazaheptadecanoyl)- 4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Biological ActivityMZ 1 is a cell penetrant Degrader (PROTAC®) based on (+)-JQ1 (Cat.No. 4499) conjugated to a von Hippel-Lindau (VHL) ligand. MZ 1 induces preferential degradation of BRD4 over BRD2 and BRD3 (DC50 values for degradation of BRD4 are 8 and 23 nM in H661 and H838 cells, respectively), while retaining high affinity for BRD2, BRD3 and BRD4 bromodomains (Kd = 13-60 nM). MZ 1 induces complete degradation of BRD4 at a concentration of 100 nM, whereas complete degradation of BRD2/3 is achieved at 2 μM. Potent cytotoxicity and antiproliferative effects are exhibited in AML cell lines (pEC50 = 7.6 in Mv4-11 cells).
Negative control cis MZ 1 also available.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Application of MZ 1 in HeLa Cells. Western Blot data showing knockdown of BRD4 long isoform after MZ-1 (Cat. No. 6154, 1 μM) treatment of HeLa cells. Protein quantification (relative to DMSO-only control) is shown beneath the corresponding lane.BRD4 antibody is CST#13440 used at 1:2000 dilution. Secondary is Anti-Rabbit HAF008, 1:1000, R&D Systems. GAPDH primary antibody is R&D Systems AF5718 used at 5μg/mL. Secondary is Anti-Goat HAF017, 1:1000, R&D Systems. Data courtesy of Jeff Cooper, Bio-Techne.
External Portal InformationChemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of MZ 1 is reviewed on the Chemical Probes website.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Selective small molecule induced degradation of the BET bromodomain protein BRD4.
Zengerle et al.
ACS Chem.Biol., 2015;10:1770
Structural basis of PROTAC cooperative recognition for selective protein degradation.
Gadd et al.
A " click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation.
Wurz et al.
Citations for MZ 1
The citations listed below are publications that use Tocris products. Selected citations for MZ 1 include:
6 Citations: Showing 1 - 6
Engineered PROTAC-CID systems for mammalian inducible gene regulation
Authors: Ma Et al.
J Am Chem Soc 2023;
Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells.
Authors: Kaji Et al.
Sci Rep 2020;10:3088
BET protein targeting suppresses the PD-1/PD-L1 pathway in triple-negative breast cancer and elicits anti-tumor immune response.
Authors: Andrieu Et al.
Cancer Lett 2019;465:45
Activity of BET-proteolysis targeting chimeric (PROTAC) compounds in triple negative breast cancer.
Authors: Noblejas-Lopez Et al.
J Exp Clin Cancer Res 2019;38:383
Targeting bromodomain-containing protein 4 (BRD4) inhibits MYC expression in colorectal cancer cells.
Authors: Otto Et al.
Apabetalone (RVX-208) reduces vascular inflammation in vitro and in CVD patients by a BET-dependent epigenetic mechanism.
Authors: Tsujikawa Et al.
Clin Epigenetics 2019;11:102
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