SML2457
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
InChI
1S/C19H19ClN4O/c20-15-12-22-18(21)23-17(15)24-10-6-14-4-3-13(11-16(14)24)5-9-19(25)7-1-2-8-19/h3-4,11-12,25H,1-2,6-8,10H2,(H2,21,22,23)
InChI key
KJIQYGRWNLGGMI-UHFFFAOYSA-N
SMILES string
NC1=NC=C(C(N2CCC3=C2C=C(C=C3)C#CC4(CCCC4)O)=N1)Cl
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
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).
NF-κB-inducing kinase (NIK) inhibitor that selectively disrupts noncanonical over canonical NF-κB activation.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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