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MZ1

Chemical Structure : MZ1

CAS No.: 1797406-69-9

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MZ1 (MZ-1; BRD4 PROTAC MZ1)

Catalog No.: PC-60099Not For Human Use, Lab Use Only.

MZ1 is a PROTAC that tethers JQ1 to a ligand for the E3 ubiquitin ligase VHL, triggers and induces degradation of the BET bromodomain BRD4.

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10 mg $128 In stock
25 mg $218 In stock
50 mg $378 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

MZ1 is a PROTAC that tethers JQ1 to a ligand for the E3 ubiquitin ligase VHL, triggers and induces degradation of the BET bromodomain BRD4.
MZ1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3.
MZ1 shows Kd values of of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively.
 

Physicochemical Properties

M.Wt 1002.644
Formula C49H60ClN9O8S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(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

References

1. Zengerle M, et al. ACS Chem Biol. 2015 Aug 21;10(8):1770-7.

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