MZ 1

Biological Activity

MZ 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 (K_d = 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.

External Portal Information

Chemicalprobes.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.

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Technical Data

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.

Additional Information

Background References

1. Selective small molecule induced degradation of the BET bromodomain protein BRD4.
   Zengerle et al.
   ACS Chem.Biol., 2015;10:1770
2. Structural basis of PROTAC cooperative recognition for selective protein degradation.
   Gadd et al.
   Nat.Chem.Biol., 2017;
3. A " click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation.
   Wurz et al.
   J.Med.Chem., 2017;

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