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说明： (+)-JQ1 based Degrader (PROTAC®) that preferentially degrades BRD4
化学名： (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
纯度： ≥98% (HPLC)
生物活性 for MZ 1
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 (Kd = 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.
Scientific Data
Western Blot
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Application of MZ 1 in HeLa Cells. Western Blot data showing knockdown of BRD4 long isoform after MZ-1 (Catalog # 6154, 1 μM) treatment of HeLa cells. Protein quantification (relative to DMSO-only control) is shown beneath the corresponding lane. BRD4 antibody is CST#13440 used at 1:2000 dilution. Secondary is Anti-Rabbit HAF008, 1:1000, R&D Systems. GAPDH primary antibody is R&D Systems AF5718 used at 5μg/mL. Secondary is Anti-Goat HAF017, 1:1000, R&D Systems. Data courtesy of Jeff Cooper, Bio-Techne.
许可信息
Sold under licence from the University of Dundee
External Portal Information for MZ 1
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.
技术数据 for MZ 1
| 分子量 | 1002.64 |
| 公式 | C49H60ClN9O8S2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1797406-69-9 |
| PubChem ID | 122201421 |
| InChI Key | PTAMRJLIOCHJMQ-PYNGZGNASA-N |
| Smiles | CC1=C(C2=C(N3C(C)=NN=C3[C@@H](N=C2C4=CC=C(C=C4)Cl)CC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5C[C@@H](C[C@H]5C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)O)=O)=O)=O)S1)C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for MZ 1
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 100.26 | 100 | |
| ethanol | 100.26 | 100 |
制备储备液 for MZ 1
以下数据基于产品分子量 1002.64。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1 mL | 4.99 mL | 9.97 mL |
| 5 mM | 0.2 mL | 1 mL | 1.99 mL |
| 10 mM | 0.1 mL | 0.5 mL | 1 mL |
| 50 mM | 0.02 mL | 0.1 mL | 0.2 mL |
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产品说明书 for MZ 1
参考文献 for MZ 1
参考文献是支持产品生物活性的出版物。
Zengerle et al (2015) Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS.Chem.Biol 10 1770 PMID: 26035625
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
Zhou et al (2022) A comprehensive review of BET-targeting PROTACs for cancer therapy. Bioorg.Med.Chem. 73 117033 PMID: 36202064
If you know of a relevant reference for MZ 1, please let us know.
关键词: MZ 1, MZ 1 supplier, MZ1, PROTAC, PROTACs, Proteolysis, targeted, chimeras, Bromodomain, BRD2, BRD3, BRD4, BET, proteins, JQ1, VHL, E3, ubiquitin, ligase, HIF-alpha, HIF-a, HIF-α, active, degraders, degrades, protein, degradation, tpd, Bromodomains, (BRD), Degraders, 6154, Tocris Bioscience
8 篇 MZ 1 的引用文献
引用文献是使用了 Tocris 产品的出版物。 MZ 1 的部分引用包括：
Noblejas-Lopez et al (2019) Activity of BET-proteolysis targeting chimeric (PROTAC) compounds in triple negative breast cancer. J Exp Clin Cancer Res 38 383 PMID: 31470872
Andrieu et al (2019) BET protein targeting suppresses the PD-1/PD-L1 pathway in triple-negative breast cancer and elicits anti-tumor immune response. Cancer Lett 465 45 PMID: 31473251
Tsujikawa et al (2019) Apabetalone (RVX-208) reduces vascular inflammation in vitro and in CVD patients by a BET-dependent epigenetic mechanism. Clin Epigenetics 11 102 PMID: 31300040
Otto et al (2019) Targeting bromodomain-containing protein 4 (BRD4) inhibits MYC expression in colorectal cancer cells. Neoplasia 21 1110 PMID: 31734632
Ma et al (2023) Engineered PROTAC-CID systems for mammalian inducible gene regulation J Am Chem Soc 145 1593 PMID: 36626587
Kristin M et al (2021) Kinetic Detection of E3:PROTAC:Target Ternary Complexes Using NanoBRET Technology in Live Cells. Methods Mol Biol 2365 151-171 PMID: 34432243
Philippe et al (2020) Endoplasmic reticulum stress actively suppresses hepatic molecular identity in damaged liver. Mol Syst Biol 16 e9156 PMID: 32407006
Kaji et al (2020) Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells. Sci Rep 10 3088 PMID: 32080280
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
TPD and Induced Proximity Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia