| Identification | Back Directory | [Name]
Imidazo[1,2-b]pyridazin-6-amine, 3-(1H-indazol-6-yl)-N-methyl-N-(tetrahydro-2H-pyran-4-yl)- | [CAS]
2727872-68-4 | [Synonyms]
SRI-42127
Imidazo[1,2-b]pyridazin-6-amine, 3-(1H-indazol-6-yl)-N-methyl-N-(tetrahydro-2H-pyran-4-yl)- | [Molecular Formula]
C19H20N6O | [MOL File]
2727872-68-4.mol | [Molecular Weight]
348.4 |
| Chemical Properties | Back Directory | [density ]
1.44±0.1 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
DMSO: 2mg/mL, clear (warmed) | [form ]
Solid | [pka]
12.99±0.40(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
SRI-42127 is a HuR translocation inhibitor. HuR is an RNA regulator that binds to AREs, and HuR translocations promote the production of inflammatory cytokines in glial cells. However, SRI-42127 can destroy mRNA stability and inhibit gene promoter activation. SRI-42127 also inhibits microglial cell activation and attenuates recruitment/chemotaxis of neutrophils and monocytes[1]. | [Biological Activity]
SRI-42127 is a blood-brain barrier permeable imidazopyridazinamine analog th at potently and reversibly inhibits the RNA-binding protein HuR multimerization and blocks HuR nucleocytoplasmic shuttling. SRI-42127 suppresses the expression and release of several pro-inflammatory mediators with minimal effect on anti-inflammatory cytokines. SRI 42127 weakens HuR interaction with Bcl-2 and Mcl-1 leading to induction of apoptosis and decreased tumor growth. SRI42127 subdues microglial activation in vivo and attenuates the recruitment/chemotaxis of neutrophils and monocytes. | [in vivo]
SRI-42127 (15 mg/kg; i.p.; single dose) suppresses HuR translocation and the activation of microglia in mice model[1].
| [References]
[1] Chellappan R, et al. SRI-42127, a novel small molecule inhibitor of the RNA regulator HuR, potently attenuates glial activation in a model of lipopolysaccharide-induced neuroinflammation. Glia. 2022 Jan;70(1):155-172. DOI:10.1002/glia.24094 |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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