MZ 1

Catalog # Availability Size / Price Qty
6154/5
Cat.No. 6154 - MZ 1 | C49H60ClN9O8S2 | CAS No. 1797406-69-9
1 Image
Description: (+)-JQ1 based PROTAC that selectively degrades BRD4 in cells

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

Purity: ≥98%

Product Details
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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 (DC50 values for degradation of BRD4 are 8 and 23 nM in H661 and H838 cells, respectively). Exhibits potent cytotoxicity and antiproliferative effects in AML cell lines (pEC50 = 7.6 in Mv4-11 cells). 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.

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.

Additional Information

Licensing Caveats:
Sold under licence from the University of Dundee
Other Product-Specific Information:

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