A PROTAC that drives BRD4 degradation
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dBET57

Item No. 36626

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(6S)-4-(4-chlorophenyl)-N-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
CAS Number
1883863-52-2
Molecular Formula
C34H31ClN8O5S
Formula Weight
699.2
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
220, 260 nm
SMILES
CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@@H](CC(NCCNC4=C5C(C(N(C6C(NC(CC6)=O)=O)C5=O)=O)=CC=C4)=O)C7=NN=C(C)N27
InChi Code
InChI=1S/C34H31ClN8O5S/c1-16-17(2)49-34-27(16)29(19-7-9-20(35)10-8-19)38-23(30-41-40-18(3)42(30)34)15-26(45)37-14-13-36-22-6-4-5-21-28(22)33(48)43(32(21)47)24-11-12-25(44)39-31(24)46/h4-10,23-24,36H,11-15H2,1-3H3,(H,37,45)(H,39,44,46)/t23-,24?/m0/s1
InChi Key
CZRLOIDJCMKJHE-UXMRNZNESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $32

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    5 mg

    $141

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    10 mg

    $248

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    25 mg

    $426

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    Product Description

    dBET57 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 JQ1, which binds bromo- and extra-terminal domain (BET) proteins, linked to thalidomide, a ligand for the E3 ubiquitin ligase cereblon. dBET57 is selective for inhibiting the interaction between cereblon and bromodomain 1 of BRD4 (BRD4BD1) over the interaction between cereblon and BRD4BD2 with apparent cooperativity factor α (αapp) values of 0.8 and less than 0.1, respectively, in an assay using purified bromodomains. It reduces BRD4BD1 protein levels in vitro with a half-maximal degradation (DC50) value of approximately 500 nM after five hours but does not reduce levels of BRD4BD2.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nowak, R.P., DeAngelo, S.L., Buckley, D., et al. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat. Chem. Biol. 14(7), 706-714 (2018).