MZ 1

Cat. No. 6154new

MZ 1 C49H60ClN9O8S2 [1797406-69-9]

Price and Availability

For MZ 1 pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

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 Activity

Cell penetrant Proteolysis Targeting Chimera (PROTAC) compound based on (+)-JQ1 (Cat.No. 4499), conjugated to a von Hippel-Lindau (VHL) ligand. Retains high affinity for BRD2, BRD3 and BRD4 bromodomains (Kd = 13-60 nM) but induces preferential degradation of BRD4 over BRD2 and BRD3 in cells at 10-100 nM concentrations. DC50 values for degradation of BRD4 are 8 and 23 nM in H661 and H838 cells, respectively. Replicates the effects of BRD4 protein removal by siRNA altering downstream gene expression patterns: downregulation of MYC and upregulation of genes such as P21 and AREG. No significant effect on HIF-α stabilization when used at low concentrations (<10 μM). Exhibits potent cytotoxicity and profound antiproliferative effects in AML cell lines such as Mv4;11 (pEC50 = 7.6), more potent and more effective than (+)-JQ1 (pEC50 = 6.5). Negative control cis MZ 1 also available.

PROTACs are bi-functional small molecules that harness the ubiquitin/proteasome system (UPS) to selectively and catalytically remove target proteins from cells.

Licensing Information

Sold under licence from the University of Dundee

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.

Technical Data

M.Wt:
1002.64
Formula:
C49H60ClN9O8S2
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
1797406-69-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Gadd et al (2017) Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat.Chem.Biol.. PMID: 28288108.

Wurz et al (2017) A "click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem.. PMID: 28378579.

Zengerle et al (2015) Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS.Chem.Biol 10 1770. PMID: 26035625.

If you know of a relevant reference for MZ 1 please let us know.

Citations are publications that use Tocris products.

Do you know of a great paper that uses MZ 1 from Tocris? If so please let us know.

View Related Products by Product Action

Keywords: MZ 1, supplier, MZ1, PROTAC, Proteolysis, targeted, chimeras, Bromodomain, BRD2, BRD3, BRD4, BET, proteins, JQ1, VHL, E3, ubiquitin, ligase, HIF-alpha, HIF-a, HIF-α, Tocris Bioscience, Ubiquitin E3 Ligase products

Quick Order

Find multiple products by catalog number

divider line

Programmed Cell Death

Written by Bram van Raam and Guy Salvesen

Programmed Cell Death Life Science Poster

Our Programmed Cell Death poster gives a summary of the signaling pathways involved in apoptosis, necroptosis and cell survival. Request copy or view PDF today.

divider line

The p53 Tumor Suppressor Response

Written by Christopher J. Brown et al

p53 Life Science Poster

A summary of the main strategies for the reactivation of p53, including small molecules and peptides, which act to stabilize p53 to rescue wild-type activity. Request copy today.

divider line

New Products in this Area

cis VH 298

Negative control for VH 298

VH 298

High-affinity inhibitor of VHL

cis MZ 1

Negative Control for MZ1

Sign-up for new product e-alerts
divider line

Bio-Techne Events

ISSCR 2017

ISSCR 2017

June 14 - 17, 2017

Boston, MA, USA

Booth: 419