| Identification | Back Directory | [Name]
2-Pyridinecarboxamide, 5-[[(6-chloro-2-pyridinyl)methyl](1-oxo-2-propen-1-yl)amino]-N-phenyl- | [CAS]
2305052-86-0 | [Synonyms]
BPK-25
2-Pyridinecarboxamide, 5-[[(6-chloro-2-pyridinyl)methyl](1-oxo-2-propen-1-yl)amino]-N-phenyl- | [Molecular Formula]
C21H17ClN4O2 | [MOL File]
2305052-86-0.mol | [Molecular Weight]
392.84 |
| Chemical Properties | Back Directory | [Boiling point ]
521.1±50.0 °C(Predicted) | [density ]
1.351±0.06 g/cm3(Predicted) | [storage temp. ]
4°C, stored under nitrogen | [solubility ]
DMSO : 150 mg/mL (381.83 mM; Need ultrasonic) | [form ]
Solid | [pka]
11.53±0.70(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP[1]. | [Biological Activity]
BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP[1].
BPK-25 (10 μM; 5 hours) inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP[1]. BPK-25 (10 μM; 24 hours) suppresses NF-κB activation blocks nuclear factor of activated T-cells (NFAT) activation, as measured by >50% reductions in IκBα phosphorylation[1]. BPK-25 (10 μM; 4 hours) also reduces NFATc2 expression in T cells[1]. BPK-25 (0.1, 1, 5, 10, 20 μM; 24 hours) promotes the striking and selective reduction of several proteins in the nucleosome remodeling and deacetylation (NuRD) complex in a concentration- and time-dependent manner. BPK-25 does not have corresponding changes in mRNA expression[1]. A non-electrophilic propanamide analog of BPK-25 (BPK-25-ctrl) does not suppress T cell activation or affect NuRD complex proteins in T cells[1]. | [References]
[1]. Ekaterina V Vinogradova, et al. An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. |
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