A PROTAC that drives H-PGDS degradation
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PROTAC(H-PGDS)-7

Item No. 35561

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[4-[[4-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]-1-piperazinyl]carbonyl]-1-piperidinyl]phenyl]-2-phenoxy-5-pyrimidinecarboxamide
CAS Number
2761281-50-7
Synonyms
  • Proteolysis-targeting Chimera (Prostaglandin D Synthase (hematopoietic-type))-7
Molecular Formula
C40H38N8O7
Formula Weight
742.8
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/ml
SMILES
O=C(N1CCN(C2=C(C(N(C3C(NC(CC3)=O)=O)C4=O)=O)C4=CC=C2)CC1)C(CC5)CCN5C6=CC=C(NC(C7=CN=C(OC8=CC=CC=C8)N=C7)=O)C=C6
InChi Code
InChI=1S/C40H38N8O7/c49-33-14-13-32(36(51)44-33)48-38(53)30-7-4-8-31(34(30)39(48)54)46-19-21-47(22-20-46)37(52)25-15-17-45(18-16-25)28-11-9-27(10-12-28)43-35(50)26-23-41-40(42-24-26)55-29-5-2-1-3-6-29/h1-12,23-25,32H,13-22H2,(H,43,50)(H,44,49,51)
InChi Key
KQNXUQJGOJWQGL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    500 µg

    $217

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    1 mg

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    Product Description

    PROTAC(H-PGDS)-7 is a proteolysis-targeting chimera (PROTAC) comprised of the hematopoietic prostaglandin D synthase (H-PGDS) inhibitor TFC-007 (Item No. 17971) and the cereblon inhibitor pomalidomide (Item No. 19877).1 It induces degradation of H-PGDS in KU812 cells with a 50% degradation concentration (DC50) value of 17.3 pM, as well as decreases the production of prostaglandin D2 (PGD2) in the same cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yokoo, H., Shibata, N., Endo, A., et al. Discovery of a highly potent and selective degrader targeting hematopoietic prostaglandin D synthase via in silico design. J. Med. Chem. 64(21), 15868-15882 (2021).