A DAX1 ligand
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BPK-29 (hydrochloride)

Item No. 45897

Technical Information
Formal Name
2-chloro-N-[hexahydro-1-[4-(4-morpholinyl)benzoyl]-1H-azepin-4-yl]-N-(phenylmethyl)-acetamide, monohydrochloride
CAS Number
2444815-73-8
Molecular Formula
C26H32ClN3O3 • HCl
Formula Weight
Purity
≥98%
A solid
SMILES
O=C(N1CCC(N(C(CCl)=O)CC2=CC=CC=C2)CCC1)C3=CC=C(N4CCOCC4)C=C3.Cl
InChi Code
InChI=1S/C26H32ClN3O3.ClH/c27-19-25(31)30(20-21-5-2-1-3-6-21)24-7-4-13-29(14-12-24)26(32)22-8-10-23(11-9-22)28-15-17-33-18-16-28;/h1-3,5-6,8-11,24H,4,7,12-20H2;1H
InChi Key
FRNJMSGTTWKVPV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BPK-29 is a ligand of the orphan nuclear receptor DAX1, also known as NR0B1.1 It covalently binds to DAX1 at Cys274 and inhibits the protein-protein interaction between DAX1 and SNW1 (IC50 = ~10-20 µM) and between DAX1 and RBM45 at 30 µM. BPK-29 (5 µM) inhibits the anchorage-independent growth of KEAP1-mutant H460 non-small cell lung cancer (NSCLC) cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bar-Peled, L., Kemper, E.K., Suciu, R.M., et al. Chemical proteomics identifies druggable vulnerabilities in a genetically defined cancer. Cell 171(3), 696-709 (2017).