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Chemical Structure : NVS-BPTF-1
Catalog No.: PC-72789Not For Human Use, Lab Use Only.
NVS-BPTF-1 is the first highly potent and selective BPTF-bromodomain inhibitor with IC50 of 56 nM in an AlphaScreen assay and Kd of 71 nM in a BLI assay.
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NVS-BPTF-1 is the first highly potent and selective BPTF-bromodomain inhibitor with IC50 of 56 nM in an AlphaScreen assay and Kd of 71 nM in a BLI assay.
NVS-BPTF-1 displays no significant interaction in DSF screen and a BROMOscan against a panel of other human bromodomains.
In HEK293 cells, NVS-BPTF-1 showed on-target activity with an IC50 of 16 nM, as measured by a nanoBRET assay.
NVS-BPTF-1 did not affect the proliferation of multiple human cancer cell lines, and NVS-BPTF-1 did not affect the level of PSMB8 and PSMB9 or TAP1 and TAP2, unlike BPTF siRNA knockdown caused effect.
| M.Wt | 537.614 | |
| Formula | C26H28FN7O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Léa Mélin, et al. Bioorg Med Chem Lett. 2021 Sep 1;47:128208.
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