检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
NC1=NC=C(C(N2CCC3=C2C=C(C=C3)C#CC4(CCCC4)O)=N1)Cl
生化/生理作用
Amgen16 is an NF-κB-inducing kinase (NIK) inhibitor that selectively disrupts noncanonical NF-κB activation in U-2 OS cells (lymphotoxin β receptor LTβR-/TWEAK recetor FN14-mediated p52 nuclear translocation IC50 = 417 nM/2.517 μM) without affecting canonical NF-κB activation (TNF-α-stimulated p65 (RelA) nuclear translocation IC50 >30 μM). Likewise, Amgen16 (1 μM, 30 min pretreatment) selectively inhibits NFKB2 (p100) mRNA production upon noncanonical NF-κB activation (by 84%; 20 ng/mL TWEAK for 4 h), while exhibiting much smaller effect against canonical NF-κB stimulator-induced NFKB2 production (by 36%; 10 ng/mLTNFα for 4 h).
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Science signaling, 11(541) (2018-08-02)
Members of the family of nuclear factor κB (NF-κB) transcription factors are critical for multiple cellular processes, including regulating innate and adaptive immune responses, cell proliferation, and cell survival. Canonical NF-κB complexes are retained in the cytoplasm by the inhibitory
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