| Company Name: |
Sigma-Aldrich |
| Tel: |
021-61415566 800-8193336 |
| Email: |
orderCN@merckgroup.com |
Amgen IRE1α Inhibitor manufacturers
- Kira8
-
- $89.00
-
2026-07-27
- CAS:1630086-20-2
- Purity: 99.52%
- Supply Ability: 10g
- Kira8
-
- $89.00
-
2026-07-27
- CAS:1630086-20-2
- Purity: 99.52%
- Supply Ability: 10g
|
| | Amgen IRE1α Inhibitor Basic information |
| Product Name: | Amgen IRE1α Inhibitor | | Synonyms: | Amgen IRE1α Inhibitor;Kira8;IRE-1 INHIBITOR;KIRA8 (AMG-18);Benzenesulfonamide, 2-chloro-N-[6-methyl-5-[[3-[2-[(3S)-3-piperidinylamino]-4-pyrimidinyl]-2-pyridinyl]oxy]-1-naphthalenyl]-;(S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide;Amgen IRE1a Inhibitor;Inositol requiring enzyme 1,inhibit,AMG18,AMG 18,Kira 8,Kira8,Inhibitor,IRE1,Kira-8 | | CAS: | 1630086-20-2 | | MF: | C31H29ClN6O3S | | MW: | 601.12 | | EINECS: | | | Product Categories: | | | Mol File: | 1630086-20-2.mol |  |
| | Amgen IRE1α Inhibitor Chemical Properties |
| 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 | | InChIKey | XMWUCMFVDXDRDE-NRFANRHFSA-N | | SMILES | [S](=O)(=O)(Nc2c3c(c(c(cc3)C)Oc4ncccc4c5nc(ncc5)N[C@@H]6CNCCC6)ccc2)c1c(cccc1)Cl |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | Amgen IRE1α Inhibitor Usage And Synthesis |
| 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-competitive, potent 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 fibrosis, multiple 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. |
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| | Amgen IRE1α Inhibitor Preparation Products And Raw materials |
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