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Merck

SML2457

Sigma-Aldrich

Amgen16

≥98% (HPLC)

别名:

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

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About This Item

经验公式(希尔记法):
C19H19ClN4O
分子量:
354.83
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

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).

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Kate L Henry et al.
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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