A hybrid molecule containing (+)-JQ-1 and thalidomide
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dBET1

Item No. 18044

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(6S)-4-(4-chlorophenyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
CAS Number
1799711-21-9
Molecular Formula
C38H37ClN8O7S
Formula Weight
785.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlDMSO:PBS (pH 7.2)(1:5): 0.16 mg/mlEthanol: 5 mg/ml
λmax
218, 254, 323 nm
SMILES
CC1=NN=C2[C@H](CC(NCCCCNC(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/C38H37ClN8O7S/c1-19-20(2)55-38-31(19)33(22-9-11-23(39)12-10-22)42-25(34-45-44-21(3)46(34)38)17-29(49)40-15-4-5-16-41-30(50)18-54-27-8-6-7-24-32(27)37(53)47(36(24)52)26-13-14-28(48)43-35(26)51/h6-12,25-26H,4-5,13-18H2,1-3H3,(H,40,49)(H,41,50)
InChi Key
LKEGXJXRNBALBV-PMCHYTPCSA-N
License
Sold under license from Dana-Farber Cancer Institute, Inc.
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $49

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    5 mg

    $213

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    10 mg

    $400

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    Cayman Chemical
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    Product Description

    dBET1 is a hybrid molecule that combines (+)-JQ1 (Item No. 11187) and thalidomide (Item No. 14610).1 The JQ1 portion facilitates binding of dBET1 to the bromodomains of BET family transcriptional activators. The thalidomide moiety drives proteasomal degradation, as phthalimides bind cereblon to create a substrate recognition site for E3 protein ligase complex-mediated ubiquitination. dBET1 induces cereblon-dependent BET protein degradation in vitro (EC50 = 430 nM) and in vivo and delays leukemia progression in mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Winter, G.E., Bucklet, D.L., Paulk, J., et al. Phthalimide conjugation as a strategy for in vivo target protein degradation. Sciencexpress 1-9 (2015).