SMARCA2/SMARCA4 ligand-1 

SMARCA2/SMARCA4 ligand-1 is a SMARCA2/SMARCA4 ligand with K_D values of 1.2 and 10.3 nM. SMARCA2/SMARCA4 ligand-1 binds SMARCA2/4 bromodomain via hydrogen bonds with asparagine and tyrosine residues, and a salt bridge with a glutamate residue. SMARCA2/SMARCA4 ligand-1 shows antiproliferative activity against cancer cells. SMARCA2/SMARCA4 ligand-1 can be used for the research of cancer, such as smarca4 mutant nonsmall cell lung cancer^[1].

SMARCA2/SMARCA4 ligand-1 (Compound 4p) potently binds to purified SMARCA2 bromodomain with an IC₅₀ of 95.8 nM^[1].
SMARCA2/SMARCA4 ligand-1 binds to purified SMARCA4 bromodomain with potency with an IC₅₀ of 285 nM^[1].
SMARCA2/SMARCA4 ligand-1(0.064-200 μM) binds to purified SMARCA2 bromodomain with a K_d of 1.2 nM^[1].
SMARCA2/SMARCA4 ligand-1 (0.625-10 μM) binds to purified SMARCA4 bromodomain with a K_d of 10.3 nM^[1].
SMARCA2/SMARCA4 ligand-1 demonstrates high stability in aqueous solutions at pH 1 and pH 7 and in cell culture medium, retaining >99% purity over 24 h^[1].
SMARCA2/SMARCA4 ligand-1 (compound 4p) shows antiproliferative activity in NCI-H1568 and HEK-293 cells with IC₅₀ values of 13.94 and 11.76 μM^[1].
SMARCA2/SMARCA4 ligand-1 (20 μM; 2 h) rescues SMARCA2 and PBRM1 in NCI-H1568 cells, confirming target engagement dependency of the PROTAC effect^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

409.28

C₂₀H₁₇BrN₄O

O=C1[N-][N+]2=CC3=CC=C(C=C3C=C2C4=CC=CC(Br)=C14)N5CCNCC5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zhang S, et al. N-Iminopyridinium Ylides as Chemically Stable Pharmacophores Enabling Targeted Degradation of SMARCA Proteins[J]. JACS Au, 2026.