| Identification | Back Directory | [Name]
Amgen IRE1α Inhibitor | [CAS]
1630086-20-2 | [Synonyms]
Kira8
KIRA8 (AMG-18)
IRE-1 INHIBITOR
Amgen IRE1α Inhibitor
Benzenesulfonamide, 2-chloro-N-[6-methyl-5-[[3-[2-[(3S)-3-piperidinylamino]-4-pyrimidinyl]-2-pyridinyl]oxy]-1-naphthalenyl]- | [Molecular Formula]
C31H29ClN6O3S | [MDL Number]
MFCD28404657 | [MOL File]
1630086-20-2.mol | [Molecular Weight]
601.12 |
| Chemical Properties | Back Directory | [Boiling point ]
812.6±75.0 °C(Predicted) | [density ]
1.383±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Water:30.0(Max Conc. mg/mL);49.91(Max Conc. mM) | [form ]
Solid | [pka]
7.66±0.30(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Amgen IRE1α Inhibitor is an inhibitor of IRE1α. IRE1α is a sensor of unfolded protein accumulation that triggers the unfolded protein response. | [Biological Activity]
KIRA8 is an ATP-competitivepotent and selective IRE1α kinase inhibitor (IRE1α/β Ki = 2/120 nM) th at 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 fibrosismultiple myeloma (MM)and pancreatic neuroendocrine tumors (PanNET) in vivo (30-50 mg/kg/day i.p.). | [in vivo]
Male Ins2+/Akita mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), significant reduction of hyperglycemia become apparent over several weeks[1].
?
One week treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserves Ins1/Ins2, BiP and MANF mRNAs[1]. | Animal Model: | Male Ins2+/Akita mice[1] | | Dosage: | 50 mg/kg | | Administration: | Injected i.p.; daily; for 35 days | | Result: | Significant reduction of hyperglycemia became apparent over several weeks. |
|
|
| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|