2662454-54-6
2662454-54-6 structure
- Name: NVS-BPTF-1
- Chemical Name: NVS-BPTF-1
- CAS Number: 2662454-54-6
- Molecular Formula: C26H28FN7O3S
- Molecular Weight: 537.614
- Create Date: 2022-07-01 17:43:19
- Modify Date: 2024-04-07 22:25:09
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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.
| Name | NVS-BPTF-1 |
|---|
| Description | 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. |
|---|---|
| References | 1. Léa Mélin, et al. Bioorg Med Chem Lett. 2021 Sep 1;47:128208. |
| Molecular Formula | C26H28FN7O3S |
|---|---|
| Molecular Weight | 537.614 |