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Amgen IRE1α Inhibitor

Product Name
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
Formula Weight
601.12
MOL File
1630086-20-2.mol
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Amgen IRE1α Inhibitor Property

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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
VBP00322
Product name
(S)-2-chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide
Purity
Aldrich<SUP>CPR</SUP>
Packaging
10 mg
Price
$1420
Updated
2025/07/31
TRC
Product number
A576530
Product name
AmgenIRE1αInhibitor
Packaging
10mg
Price
$1320
Updated
2021/12/16
ChemScene
Product number
CS-0084229
Product name
Kira8
Purity
99.74%
Packaging
5mg
Price
$320
Updated
2021/12/16
ChemScene
Product number
CS-0084229
Product name
Kira8
Purity
99.74%
Packaging
10mg
Price
$520
Updated
2021/12/16
Crysdot
Product number
CD11242815
Product name
(S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide
Purity
97%
Packaging
5mg
Price
$689
Updated
2021/12/16
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Amgen IRE1α Inhibitor Chemical Properties,Usage,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

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Amgen IRE1α Inhibitor Suppliers

Canada 1 China 41 India 1 United States 7 Global 50
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
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marketing@targetmol.com
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United States
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32435
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InvivoChem
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+1-708-310-1919 +1-13798911105
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708-557-7486
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sales@invivochem.cn
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United States
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TargetMol Chemicals Inc.
Tel
+1-781-999-5354;
Email
support@targetmol.com
Country
United States
ProdList
39035
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58
Aladdin Scientific
Tel
Email
tp@aladdinsci.com
Country
United States
ProdList
52923
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United States Biological
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chemicals@usbio.net
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United States
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MedChemExpress
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sales@medchemexpress.com
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United States
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6398
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AstaTech, Inc
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Email
sales@astatechinc.com
Country
United States
ProdList
6371
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1630086-20-2, Amgen IRE1α InhibitorRelated Search:


  • Kira8
  • Amgen IRE1α Inhibitor
  • 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
  • (S)-2-Chloro-N-[6-methyl-5-[[3-[2-(3-piperidylamino)-4-pyrimidinyl]-2-pyridyl]oxy]-1-naphthyl]benzenesulfonamide
  • Kira8, 10 mM in DMSO
  • Amgen IRE1± Inhibitor
  • Kira8 ，E2652
  • 1630086-20-2
  • C31H29ClN6O3S