cis-MZ 1 hydrate 

cis-MZ 1 hydrate serves as a negative control for BRD4-targeted PROTAC MZ 1 (HY-107425). cis-MZ 1 hydrate can be used in colorectal cancer-related research^[1][2][3]. (Pink: BRD4 ligand (HY-13030); Blue: VHL ligand (HY-120217A); Black: linker (HY-42637)).

cis-MZ 1 hydrate shows no detectable binding affinity to the VHL-ElonginB-ElonginC complex in in vitro ITC experiments^[1].
cis-MZ 1 (1 μM; 24-36 h) hydrate does not induce the degradation of BRD2, BRD3, or BRD4 in HeLa cells^[1].
cis-MZ 1 (5 μM; up to 4 h) hydrate does not induce degradation of GFP-tagged BRD4 in U2OS cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1007.15

C₄₉H₆₀ClN₉O₈S₂.1/4H₂O

Solid

White to off-white

CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@@H](CC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](C4)O)C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)=O)=O)=O)C7=NN=C(C)N27.[0.25].O

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Zengerle M, et al. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. ACS Chem Biol. 2015;10(8):1770-1777.  [Content Brief]

  [2]. Gadd MS, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017;13(5):514-521.  [Content Brief]

  [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.