SML2457

Amgen16

≥98% (HPLC)

• Synonym(e): 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
• Empirische Formel (Hill-System): C₁₉H₁₉ClN₄O
• CAS-Nummer: 1202761-92-9
• Molekulargewicht: 354.83
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: 2-8°C
• SMILES String: NC1=NC=C(C(N2CCC3=C2C=C(C=C3)C#CC4(CCCC4)O)=N1)Cl

Beschreibung

Biochem./physiol. Wirkung

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).

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable