Synonyms: 1-((1-(2-Amino-5-chloropyrimidin-4-yl)indolin-6-yl)ethynyl)cyclopentanol; 1-[2-[1-(2-Amino-5-chloro-4-pyrimidinyl)-2,3-dihydro-1H-indol-6-yl]ethynyl]cyclopentanol; Amgen 16
Molecular Formula: C19H19ClN4O
Molecular Weight: 354.83
Linear Structural Formula: C19H19ClN4O
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: Amgen16 is an NF-kappaB-inducing kinase (NIK) inhibitor that selectively disrupts noncanonical NF-kappaB activation in U-2 OS cells (lymphotoxin beta receptor LTbetaR-/TWEAK recetor FN14-mediated p52 nuclear translocation IC50 = 417 nM/2.517 muM) without affecting canonical NF-kappaB activation (TNF-alpha-stimulated p65 (RelA) nuclear translocation IC50 >30 muM). Likewise, Amgen16 (1 muM, 30 min pretreatment) selectively inhibits NFKB2 (p100) mRNA production upon noncanonical NF-kappaB activation (by 84%; 20 ng/mL TWEAK for 4 h), while exhibiting much smaller effect against canonical NF-kappaB stimulator-induced NFKB2 production (by 36%; 10 ng/mLTNFalpha for 4 h).