A PBRM1, BRM, and BRG1 ligand
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SMARCA-BD Ligand 1 for PROTAC (hydrochloride)

Item No. 45620

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[6-amino-5-(1-piperazinyl)-3-pyridazinyl]-phenol, dihydrochloride
CAS Number
2369053-68-7
Synonyms
  • SMARCA-BD Ligand 1 for Proteolysis-targeting Chimera
Molecular Formula
C14H17N5O • 2HCl
Formula Weight
344.2
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
OC1=CC=CC=C1C2=CC(N3CCNCC3)=C(N=N2)N.Cl.Cl
InChi Code
InChI=1S/C14H17N5O.2ClH/c15-14-12(19-7-5-16-6-8-19)9-11(17-18-14)10-3-1-2-4-13(10)20;;/h1-4,9,16,20H,5-8H2,(H2,15,18);2*1H
InChi Key
INBBYNMFULAIMY-UHFFFAOYSA-N
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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    5 mg

    $175

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    10 mg

    $280

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    Product Description

    SMARCA-BD ligand 1 for PROTAC is a ligand for polybromo-1D (PBRM1), Brahma homolog (BRM), also known as SMARCA2, and Brahma-related gene 1 (BRG1), also known as SMARCA4 (Kds = 26, 135, and 73 nM, respectively).1 SMARCA-BD ligand 1 for PROTAC has been used in the synthesis of the proteolysis-targeting chimeras (PROTACs) AU-15330 (Item No. 43318) and ACBI1 (Item No. 36612) that induce the degradation of BRM, BRG1, and PBRM1 in cancer cells.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wanior, M., Preuss, F., Ni, X., et al. Pan-SMARCA/PB1 bromodomain inhibitors and their role in regulating adipogenesis. J. Med. Chem. 63(23), 14680-14699 (2020).

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

    3. Farnaby, W., Koegl, M., Roy, M.J., et al. BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design. Nat. Chem. Biol. 15(7), 672-680 (2019).