BAZ1A-IN-1

• CAT Number: I045222
• CAS Number: 941521-45-5
• Molecular Formula: C16H12N4O3S
• Molecular Weight: 340.36
• Purity: ≥95%
• Synonyms: 1-(3-nitrophenyl)-3-(4-phenyl-1,3-thiazol-2-yl)urea
• InChI: InChI=1S/C16H12N4O3S/c21-15(17-12-7-4-8-13(9-12)20(22)23)19-16-18-14(10-24-16)11-5-2-1-3-6-11/h1-10H,(H2,17,18,19,21)
• InChIKey: UJRJAZDAWUSWRK-UHFFFAOYSA-N
• SMILES: C1=CC=C(C=C1)C2=CSC(=N2)NC(=O)NC3=CC(=CC=C3)[N+](=O)[O-]

BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein). BAZ1A-IN-1 shows a KD value of 0.52 μM against BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A[1].
BAZ1A-IN-1 (Cpd-2) (0.015-100 μM; 96 hours) exhibits good anti-viability activity against all the four cancer cell lines that have a high expression level of BAZ1A, with IC50 values of 5.08 μM, 4.29 μM, 10.65 μM, and 7.70 μM for THP-1, ZR-75-30, BT474, and H1975 cells, respectively[1].

Reference

[1]. Yang Z, et al. Discovery of BAZ1A bromodomain inhibitors with the aid of virtual screening and activity evaluation. Bioorg Med Chem Lett. 2021;33:127745.
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