A PROTAC that drives BRD4 degradation
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dBET6

Item No. 35385

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(6S)-4-(4-chlorophenyl)-N-[8-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]octyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
CAS Number
1950634-92-0
Molecular Formula
C42H45ClN8O7S
Formula Weight
841.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 10 mg/mlEthanol: 5 mg/ml
λmax
219, 254 nm
SMILES
CC1=NN=C2[C@H](CC(NCCCCCCCCNC(COC3=CC=CC(C(N4C5C(NC(CC5)=O)=O)=O)=C3C4=O)=O)=O)N=C(C6=CC=C(Cl)C=C6)C7=C(SC(C)=C7C)N21
InChi Code
InChI=1S/C42H45ClN8O7S/c1-23-24(2)59-42-35(23)37(26-13-15-27(43)16-14-26)46-29(38-49-48-25(3)50(38)42)21-33(53)44-19-8-6-4-5-7-9-20-45-34(54)22-58-31-12-10-11-28-36(31)41(57)51(40(28)56)30-17-18-32(52)47-39(30)55/h10-16,29-30H,4-9,17-22H2,1-3H3,(H,44,53)(H,45,54)(H,47,52,55)/t29-,30?/m0/s1
InChi Key
JGQPZPLJOBHHBK-UFXYQILXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    dBET6 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 (BET) proteins, linked to thalidomide, a ligand for the E3 ubiquitin ligase cereblon.2 dBET6 binds to BRD4 (IC50 = 14 nM) and induces its degradation when used at a concentration of 100 nM, leading to a global inhibition of transcription in MOLT-4 T cell acute lymphoblastic leukemia (T-ALL) cells.1 It also reduces leukemic burden in a MOLT-4 T-ALL mouse xenograft model when administered at a dose of 7.5 mg/kg twice per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Winter, G.E., Mayer, A., Buckley, D.L., et al. BET bromodomain proteins function as master transcription elongation factors independent of CDK9 recruitment. Mol. Cell 67(1), 5-18 (2017).

    2. Goracci, L., Desantis, J., Valeri, A., et al. Understanding the metabolism of proteolysis targeting chimeras (PROTACs): The next step toward pharmaceutical applications. J. Med. Chem. 63(20), 11615-11638 (2020).