Amgen IRE1α Inhibitor
- CAS No.
- 1630086-20-2
- Chemical Name:
- Amgen IRE1α Inhibitor
- Synonyms
- Kira8;Kira8 ，E2652;KIRA8 (AMG-18);IRE-1 INHIBITOR;Kira8, 10 mM in DMSO;Amgen IRE1± Inhibitor;Amgen IRE1α Inhibitor;Amgen IRE1a Inhibitor;Inositol requiring enzyme 1,inhibit,AMG18,AMG 18,Kira 8,Kira8,Inhibitor,IRE1,Kira-8;(S)-2-Chloro-N-[6-methyl-5-[[3-[2-(3-piperidylamino)-4-pyrimidinyl]-2-pyridyl]oxy]-1-naphthyl]benzenesulfonamide
- CBNumber:
- CB73123772
- Molecular Formula:
- C31H29ClN6O3S
- Molecular Weight:
- 601.12
- MDL Number:
- MFCD28404657
- MOL File:
- 1630086-20-2.mol
| Product description | Number | Pack Size | Price |
| (S)-2-chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide AldrichCPR | VBP00322 | 10 mg | $1420 |
| AmgenIRE1αInhibitor | A576530 | 10mg | $1320 |
| Kira8 99.74% | CS-0084229 | 5mg | $320 |
| Kira8 99.74% | CS-0084229 | 10mg | $520 |
| (S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide 97% | CD11242815 | 5mg | $689 |
| 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 |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
Amgen IRE1α Inhibitor price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | VBP00322 | (S)-2-chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide AldrichCPR | 10 mg | $1420 | 2025-07-31 | Buy | |
| TRC | A576530 | AmgenIRE1αInhibitor | 1630086-20-2 | 10mg | $1320 | 2021-12-16 | Buy |
| ChemScene | CS-0084229 | Kira8 99.74% | 1630086-20-2 | 5mg | $320 | 2021-12-16 | Buy |
| ChemScene | CS-0084229 | Kira8 99.74% | 1630086-20-2 | 10mg | $520 | 2021-12-16 | Buy |
| Crysdot | CD11242815 | (S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide 97% | 1630086-20-2 | 5mg | $689 | 2021-12-16 | Buy |
Amgen IRE1α Inhibitor Chemical Properties,Uses,Production
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. |
Amgen IRE1α Inhibitor Preparation Products And Raw materials
Raw materials
Preparation Products
Amgen IRE1α Inhibitor Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32470 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3135 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39042 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 52923 | 58 | |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 18149758185; | sales-cpd@caerulumpharma.com | China | 3505 | 58 |
| Sigma-Aldrich | 021-61415566 800-8193336 | orderCN@merckgroup.com | China | 51395 | 80 |
| Chengdu Saint - Kay Biotechnology Co., Ltd. | 028-85157043 15882256948 | 676046971@qq.com | China | 4181 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11218 | 58 |
| Shanghai hongqu biomedical technology co. LTD | 88888888888 | hongquchem@qq.com | China | 5132 | 58 |
