A PROTAC that drives WDR5 degradation
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Homer

Item No. 41325

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(4'-((5-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-5-oxopentyl)carbamoyl)-4-(4-methylpiperazin-1-yl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
CAS Number
2737222-94-3
Molecular Formula
C52H60F3N9O7S
Formula Weight
1012.2
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/mLDMSO: Sparingly Soluble: 1-10 mg/mLMethanol: Slightly Soluble: 0.1-1 mg/mL
SMILES
O=C(C(C(C(F)(F)F)=C1)=CNC1=O)NC2=C(N(CC3)CCN3C)C=CC(C(C=C4)=CC=C4C(NCCCCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)=O)=C2
InChi Code
InChI=1S/C52H60F3N9O7S/c1-31-45(72-30-59-31)34-11-9-32(10-12-34)27-58-49(70)42-25-37(65)29-64(42)50(71)46(51(2,3)4)61-43(66)8-6-7-19-56-47(68)35-15-13-33(14-16-35)36-17-18-41(63-22-20-62(5)21-23-63)40(24-36)60-48(69)38-28-57-44(67)26-39(38)52(53,54)55/h9-18,24,26,28,30,37,42,46,65H,6-8,19-23,25,27,29H2,1-5H3,(H,56,68)(H,57,67)(H,58,70)(H,60,69)(H,61,66)/t37-,42+,46-/m1/s1
InChi Key
OFNZESNEBSQKSE-BQGOKDIQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $33

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    5 mg

    $158

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    Product Description

    Homer is a proteolysis-targeting chimera (PROTAC) composed of the probe for WD repeat domain 5 (WDR5) OICR-9429 (Item No. 16095) and a von Hippel-Lindau (VHL) ligand.1 It induces degradation of WDR5 in MV4-11 cells with a half-maximal degradation concentration (DC50) of 53 nM. Homer (1 µM) reduces WDR5 protein levels, but not levels of mRNA encoding WDR5, in MV4-11 cells. See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dölle, A., Adhikari, B., Krämer, A., et al. Design, synthesis, and evaluation of WD-Repeat-Containing Protein 5 (WDR5) degraders. J. Med. Chem. 64(15), 10682-10710 (2021).