A PROTAC that drives BRD4 degradation
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Diastereomer(s)
45053cis-MZ1
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MZ1

Item No. 21622

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(4R)-N-[14-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-1,13-dioxo-3,6,9-trioxa-12-azatetradec-1-yl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-L-prolinamide
CAS Number
1797406-69-9
Molecular Formula
C49H60ClN9O8S2
Formula Weight
1002.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mLDMSO: 30 mg/mLEthanol: 30 mg/mLEthanol:PBS (pH7.2) (1:7): 0.12 mg/mL
λmax
256 nm
SMILES
CC1=NN=C2[C@H](CC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N3[C@H](C(NCC4=CC=C(C5=C(C)N=CS5)C=C4)=O)C[C@@H](O)C3)=O)=O)=O)N=C(C6=CC=C(Cl)C=C6)C7=C(SC(C)=C7C)N21
InChi Code
InChI=1S/C49H60ClN9O8S2/c1-28-30(3)69-48-41(28)42(33-12-14-35(50)15-13-33)54-37(45-57-56-31(4)59(45)48)23-39(61)51-16-17-65-18-19-66-20-21-67-26-40(62)55-44(49(5,6)7)47(64)58-25-36(60)22-38(58)46(63)52-24-32-8-10-34(11-9-32)43-29(2)53-27-68-43/h8-15,27,36-38,44,60H,16-26H2,1-7H3,(H,51,61)(H,52,63)(H,55,62)/t36-,37+,38+,44-/m1/s1
InChi Key
PTAMRJLIOCHJMQ-PYNGZGNASA-N
License
Sold under license from The University of Dundee
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $53

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    1 mg

    $98

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    5 mg

    $433

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    Product Description

    MZ1 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4).1 It is characterized as a proteolysis-targeting chimera (PROTAC) and contains JQ-1, which binds bromo- and extra-terminal (BET) proteins, linked to a ligand for the E3 ubiquitin ligase VHL. MZ1 induces the selective degradation of BRD4 in HeLa cells when used at 0.1-0.5 µM.1 At concentrations of 2-10 µM, MZ1 causes the removal of BRD2, BRD3, and BRD4.1 BRD protein removal is evident within four hours of adding MZ1 and persists for at least 48 hours, unless MZ1 is removed.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zengerle, M., Chan, K.-H., and Ciulli, A. Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS Chem. Biol. 10(8), 1770-1777 (2015).