Imidazo[1,2-b]pyridazin-8-amine, 6-chloro-3-[6-fluoro-2-(phenylamino)-1H-benzimidazol-5-yl]-N-[(1-methyl-4-piperidinyl)methyl]-
![Imidazo[1,2-b]pyridazin-8-amine, 6-chloro-3-[6-fluoro-2-(phenylamino)-1H-benzimidazol-5-yl]-N-[(1-methyl-4-piperidinyl)methyl]- Structure](CAS/20210111/GIF/2328097-41-0.gif)
- CAS No.
- 2328097-41-0
- Chemical Name:
- Imidazo[1,2-b]pyridazin-8-amine, 6-chloro-3-[6-fluoro-2-(phenylamino)-1H-benzimidazol-5-yl]-N-[(1-methyl-4-piperidinyl)methyl]-
- Synonyms
- IRE1α kinase-IN-1;Imidazo[1,2-b]pyridazin-8-amine, 6-chloro-3-[6-fluoro-2-(phenylamino)-1H-benzimidazol-5-yl]-N-[(1-methyl-4-piperidinyl)methyl]-;endoribonuclease,Inositol requiring enzyme 1,cells,IRE1,oligomerization,IRE-1α kinase-IN-1,selectivity,IRE1α kinase IN 1,Inhibitor,inhibit,HEK293,autophosphorylation,reticulum,IRE1α kinaseIN1,endoplasmic
- CBNumber:
- CB08177034
- Molecular Formula:
- C26H26ClFN8
- Molecular Weight:
- 504.99
- MDL Number:
- MOL File:
- 2328097-41-0.mol
Imidazo[1,2-b]pyridazin-8-amine, 6-chloro-3-[6-fluoro-2-(phenylamino)-1H-benzimidazol-5-yl]-N-[(1-methyl-4-piperidinyl)methyl]- Chemical Properties,Uses,Production
Biological Activity
IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM)[1]. IRE1α kinase-IN-1 (compound 31) prevents endoplasmic reticulum stress-induced IRE1α oligomerization and phosphorylation, and inhibits endoribonuclease activity in human cells[1].IRE1α kinase-IN-1 and is very high selectivity with >70% inhibition of only 4/455 kinases. IRE1α kinase-IN-1 inhibits recombinant G547 IRE1α KEN domain pS274 autophosphorylation with an IC50 of 160 nM. IRE1α kinase-IN-1 inhibits tunicamycin-induced GFP-IRE1α foci in HEK293 cells with an IC50 of 0.74 μM. IRE1α kinase-IN-1 Inhibits ATP-site LanthaScreen tracer binding to recombinant dephosphorylated G547 IRE1α KEN with an IC50 of 0.27 μM[1].IRE1α kinase-IN-1 inhibits both tunicamycin- and thapsigargin-induced IRE1α-dependent splicing of XBP1 luciferase fusion mRNA in HEK293 cells with IC50s ranging 0.68-1.63 μM[1].IRE1α kinase-IN-1 (0-20 μM) inhibits IRE1α-dependent XBP1s mRNA expression in H929 cells.IRE1α kinase-IN-1 (0-20 μM) dose-dependently inhibits tunicamycin-induced expression of XBP1s in NCI-H929 cells[1].
References
[1]. Colombano G, et al. Binding to an Unusual Inactive Kinase Conformation by Highly Selective Inhibitors of Inositol-Requiring Enzyme 1α Kinase-Endoribonuclease. J Med Chem. 2019;62(5):2447-2465.
Imidazo[1,2-b]pyridazin-8-amine, 6-chloro-3-[6-fluoro-2-(phenylamino)-1H-benzimidazol-5-yl]-N-[(1-methyl-4-piperidinyl)methyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
Imidazo[1,2-b]pyridazin-8-amine, 6-chloro-3-[6-fluoro-2-(phenylamino)-1H-benzimidazol-5-yl]-N-[(1-methyl-4-piperidinyl)methyl]- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Shanghai Chaolan Chemical Technology Center | QQ:65489617 15618227136 | info@SuperLan-chem.com | China | 9767 | 58 |
| Shanghai SuperLan Chemcial Technique Centre | 021-2022843681 15618226720 | chaolaichem@foxmail.com | China | 9038 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24018 | 58 |
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