Cat. No. 6154
Chemical Name: (2S,4R)-1-((S)-2-(tert-butyl)-17-((
Biological ActivityCell 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 InformationSold under licence from the University of Dundee
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.
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.
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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
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