MZ 1

MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. Kds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively[1].

Product Specifications

CAS Number

[1797406-69-9]

UNSPSC

12352005

Hazard Statement

H315, H317, H318, H334, H335, H341, H361, H370, H413

Target

Epigenetic Reader Domain; PROTACs

Type

Reference compound

Related Pathways

Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/MZ_1.html

Purity

99.86

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC1=C(C)SC2=C1C(C3=CC=C(Cl)C=C3)=N[C@@H](CC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)=O)=O)=O)C7=NN=C(C)N27

Molecular Formula

C49H60ClN9O8S2

Molecular Weight

1002.64

Precautions

H315, H317, H318, H334, H335, H341, H361, H370, H413

References & Citations

[1]Gadd MS, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 May;13 (5) :514-521.|[2]Zengerle M, et al. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. ACS Chem Biol. 2015 Aug 21;10 (8) :1770-7.|[3]Otto C, et al. Targeting bromodomain-containing protein 4 (BRD4) inhibits MYC expression in colorectal cancer cells. Neoplasia. 2019 Nov;21 (11) :1110-1120.