A-1155463 dihydrochloride
- Parent CAS: 1235034-55-5
- Soluble in DMSO
- MF: C35H32FN5O4S2.2HCl
- MW: 742.71
Description
A-1155463 is a proteolytically stable, cell-permeable and high affinity BH3 mimetic Ligand of BCL protein BCL-XL, binding to the target potently and selectively with a Ki value of 7000-fold selectivity), BCL-W (Ki = 8 nM, >800-fold selectivity), and MCL-1 (Ki >444nM, >40000-fold selectivity). A-1155463, together with A-1331852 (Axon 3972), represent the first-in-class small molecule BCL-XL selective inhibitors achieving clear-on-target in vivo activity with high potency and selectivity. In living cells, A-1155463, as anticipated, experts an effort to disrupt the tight-binding BCL-XL-BIM, but not BCL-2–BIM, complexes, killing BCL-XL–dependent Molt-4 cells (EC50=70nM) without measurable cytotoxicity against BCL-2–dependent RS4, inducing the hallmarks of intrinsic apoptosis.
More Information
| Parent CAS No. | 1235034-55-5 |
|---|---|
| Chemical Name | 2-(8-(Benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-5-(3-(4-(3-(dimethylamino)prop-1-ynyl)-2-fluorophenoxy)propyl)thiazole-4-carboxylic acid dihydrochloride |
| extra_info | Sold in collaboration with Chemietek |
| MFCD | N.A |
| Short Description | BCL-XL selective inhibitor |
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