A PROTAC that drives BRM and BRG1 degradation
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AU-15330

Item No. 43318

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S,4R)-1-((S)-2-(2-(4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
CAS Number
2380274-50-8
Molecular Formula
C39H49N9O5S
Formula Weight
755.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O[C@H](C[C@H]1C(N[C@H](C2=CC=C(C3=C(C)N=CS3)C=C2)C)=O)CN1C([C@@H](NC(CN4CCN(C5=C(N)N=NC(C6=C(O)C=CC=C6)=C5)CC4)=O)C(C)(C)C)=O
InChi Code
InChI=1S/C39H49N9O5S/c1-23(25-10-12-26(13-11-25)34-24(2)41-22-54-34)42-37(52)31-18-27(49)20-48(31)38(53)35(39(3,4)5)43-33(51)21-46-14-16-47(17-15-46)30-19-29(44-45-36(30)40)28-8-6-7-9-32(28)50/h6-13,19,22-23,27,31,35,49-50H,14-18,20-21H2,1-5H3,(H2,40,45)(H,42,52)(H,43,51)/t23-,27+,31-,35+/m0/s1
InChi Key
HDCCMCFIGHIDJR-TUDDPRDOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $65

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    5 mg

    $293

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    10 mg

    $520

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    25 mg

    $1,055

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    Cayman Chemical
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    Product Description

    AU-15330 is a proteolysis-targeting chimera (PROTAC) that contains a von Hippel-Lindau (VHL) ligand conjugated to AU-15139, a ligand of the Brahma homolog (BHM) and Brahma-related gene 1 (BRG1), also known as SMARCA2 and SMARCA4, respectively.1 It induces degradation of BRM and BRG1 in HeLa cervical cancer cells when used at a concentration of 1 µM but also induces degradation of polybromo-1D (PBRM1) at the same concentration. AU-15330 decreases proliferation in a panel of 14 cancer cell lines (IC50s = 0.392-28.85 nM). It reduces protein levels of forkhead box protein A1 (FOXA1), ETS-related gene (ERG), Myc, and prostate-specific antigen in VCaP prostate cancer cells when used at a concentration of 1 µM for 24 hours. AU-15330 reduces tumor volume in a VCaP mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Xiao, L., Parolia, A., Qiao, Y., et al. Targeting SWI/SNF ATPases in enhancer-addicted prostate cancer. Nature 601(7893), 434-439 (2022).