BAZ1A-IN-1 |
| カタログ番号GC63694 |
BAZ1A-IN-1 は、BAZ1A (ブロモドメイン含有タンパク質) の強力な阻害剤です。 BAZ1A-IN-1 は、BAZ1A ブロモドメインに対して 0.52 μM の KD 値を示します。 BAZ1A-IN-1 は、高レベルの BAZ1A を発現するがん細胞株に対しては優れた抗生存活性を示しますが、BAZ1A の発現レベルが低いがん細胞に対しては弱いか、またはまったく活性を示しません。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 941521-45-5
Sample solution is provided at 25 µL, 10mM.
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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].
[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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