AAK1-IN-1

Biorbyt

AAK1-IN-1 [1815613-42-3]

10

1815613-42-3

Research Use Only

C19N3OF4H23

385.399

AAK1-IN-1(BMS-986176) is a chemical probe for AAK1 and BIKE that potently targets the ATP-binding site (AAK1 Ki = 9.1 nM; BIKE Ki = 17 nM). Regarding kinase selectivity, only three kinases were observed to bind SGC-AAK1-1 within 30-fold of the KD of AAK1 in a KINOMEscan assay (DiscoverX) at 1 microM followed by KD determinations: RIOK1 (KD = 72 nM), RIOK3 (KD = 290 nM), and PIP5K1C (KD = 260 nM). In a live cell NanoBRET assay (Promega) SGC-AAK1-1 has potency for ectopically expressed full-length AAK1- and BIKE-Nluc fusion proteins (AAK1 IC50 = 230 nM; BIKE IC50 = 1.5 microM).

FC(F)C1=CC(C2N=C(C(F)F)C(OC[C@@](N)(CC(C)C)C)=CC=2)=CC=N1

12352200