A PROTAC that drives kinase degradation
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DB0614

Item No. 45395

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[2-[[4-[4-[5-[[2-(2,6-dioxo-3-piperidinyl)- 2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]pentyl]-1-piperazinyl]phenyl]amino]thieno[3,2-d]pyrimidin-7-yl]phenyl]-methanesulfonamide
CAS Number
2769753-47-9
Molecular Formula
C41H42N8O7S2
Formula Weight
823.0
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
CS(=O)(NC1=CC=CC(C2=CSC3=C2N=C(N=C3)NC(C=C4)=CC=C4N(CC5)CCN5CCCCCOC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=C1)=O
InChi Code
InChI=1S/C41H42N8O7S2/c1-58(54,55)46-28-8-5-7-26(23-28)31-25-57-34-24-42-41(45-37(31)34)43-27-11-13-29(14-12-27)48-20-18-47(19-21-48)17-3-2-4-22-56-33-10-6-9-30-36(33)40(53)49(39(30)52)32-15-16-35(50)44-38(32)51/h5-14,23-25,32,46H,2-4,15-22H2,1H3,(H,42,43,45)(H,44,50,51)
InChi Key
GZRWNUKQJFXVTH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $255

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    5 mg

    $510

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    10 mg

    $638

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    Product Description

    DB0614 is a proteolysis-targeting chimera (PROTAC) containing a kinase-binding thienopyrimidine compound conjugated with the cereblon (CRBN) ligand thalidomide via an alkyl linker.1 It reduces the levels of seven kinases, NIMA-related kinase 9 (NEK9), Cdk4 and -6, AP2-associated protein kinase 1 (AAK1), proline-rich tyrosine kinase 2 (PYK2), serine/threonine kinase 17a (STK17A), and WEE1 greater than two-fold in MOLT-4 human T cell lymphoblasts at a concentration of 125 nM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ryu, S., Gadbois, G.E., Tao, A.J., et al. Synthesis and structure-activity relationships of targeted protein degraders for the understudied kinase NEK9. Curr. Res. Chem. Biol. 1, 100008 (2021).