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.

Product information

CAS Number: 2305052-86-0

Molecular Weight: 392.84

Formula: C21H17ClN4O2

Chemical Name: 5-{N-[(6-chloropyridin-2-yl)methyl]prop-2-enamido}-N-phenylpyridine-2-carboxamide

Smiles: C=CC(=O)N(CC1C=CC=C(Cl)N=1)C1=CN=C(C=C1)C(=O)NC1C=CC=CC=1

InChiKey: MHPBTJANPDDCPH-UHFFFAOYSA-N

InChi: InChI=1S/C21H17ClN4O2/c1-2-20(27)26(14-16-9-6-10-19(22)24-16)17-11-12-18(23-13-17)21(28)25-15-7-4-3-5-8-15/h2-13H,1,14H2,(H,25,28)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 150 mg/mL (381.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

BPK-25 (10 μM; 5 hours) inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP. 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. BPK-25 (10 μM; 4 hours) also reduces NFATc2 expression in T cells. 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. 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.

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