- SML2903
All Photos(1)
SML2903
KIRA8
≥98% (HPLC)
All Photos(1)
Synonym(s):
(S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide, 2-Chloro-N-[6-methyl-5-[[3-[2-[(3S)-3-piperidinylamino]-4-pyrimidinyl]-2-pyridinyl]oxy]-1-naphthalenyl]benzenesulfonamide, AMG 18, AMG-18, AMG18, Compound 18, IRE1α Kinase-Inhibiting RNase Attenuator 8
Empirical Formula (Hill Notation):
C31H29ClN6O3S
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This Item | PHL83866 | SML1459 | SML0360 |
|---|---|---|---|
| assay ≥98% (HPLC) | assay ≥95.0% (HPLC) | assay ≥98% (HPLC) | assay ≥98% (HPLC) |
| form powder | form - | form powder | form powder |
| color white to beige | color - | color white to beige | color faintly yellow to dark yellow |
| solubility DMSO: 2 mg/mL, clear | solubility - | solubility DMSO: 20 mg/mL, clear | solubility DMSO: >15 mg/mL |
| storage temp. 2-8°C | storage temp. −20°C | storage temp. 2-8°C | storage temp. 2-8°C |
| Quality Level 100 | Quality Level - | Quality Level 100 | Quality Level 100 |
生物化学的／生理学的作用
KIRA8 is an ATP-competitive, potent and selective IRE1α kinase inhibitor (IRE1α/β Ki = 2/120 nM) that attenuates IRE1α endonuclease activity (IRE1α/β IC50 = 5/55 nM) with good kinome selectivity. KIRA8 inhibits thapsigargin-induced UPR (IC50 = 99 nM; HT1080 XBP1-Luc cells) and shows therapeutic efficacy in murine models of type 1 diabetes (T1D), pulmonary fibrosis, multiple myeloma (MM), and pancreatic neuroendocrine tumors (PanNET) in vivo (30-50 mg/kg/day i.p.).
保管分類コード
11 - Combustible Solids
WGK
WGK 3
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