![]() NVS-BPTF-1 structure
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Common Name | NVS-BPTF-1 | ||
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CAS Number | 2662454-54-6 | Molecular Weight | 537.614 | |
Density | N/A | Boiling Point | N/A | |
Molecular Formula | C26H28FN7O3S | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of NVS-BPTF-1NVS-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 |
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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. |
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References | 1. Léa Mélin, et al. Bioorg Med Chem Lett. 2021 Sep 1;47:128208. |
Molecular Formula | C26H28FN7O3S |
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Molecular Weight | 537.614 |