Name | 1-(4-ethylphenyl)-3-(1H-indol-3-yl)urea |
Synonyms | H151 H-151 H 151 NEW STING inhibitor STING ANTAGONIST STING antagonist N-(4-Ethylphenyl)-N'-1H-indol-3-yl-urea 1-(4-ethylphenyl)-3-(1H-indol-3-yl)urea Urea, N-(4-ethylphenyl)-N'-1H-indol-3-yl- |
CAS | 941987-60-6 |
Molecular Formula | C17H17N3O |
Molar Mass | 279.34 |
Density | 1.298±0.06 g/cm3(Predicted) |
Boling Point | 399.9±25.0 °C(Predicted) |
Solubility | Soluble in DMSO |
Appearance | solid |
Color | Off-white |
pKa | 14.96±0.70(Predicted) |
Storage Condition | Sealed in dry,Room Temperature |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Use | H-151 is an efficient, selective and covalent STING antagonist, which can reduce phosphorylation of TBK1 and inhibit palmitoylation of human STING. |
In vitro study | H-151 (0.02-2 μM) reduces IFNβ luciferase reporter measurements of HEK293T cells. H-151 (0.5 μM; 2 h) inhibits the phosphorylation of TBK1 in THP-1 cells. H-151 (1 μM; 3 h) suppresses hsSTING palmitoylation. |
In vivo study | H-151 (750 nmol per mouse; a single i.p.) markedly reduces systemic cytokine responses in CMA-treated mice. H-151 (750 nmol per mouse; i.p. daily for 7 d) exhibits notable efficacy in Trex1 −/− mice that expressed a bioluminescent IFNβ reporter. H-151 (750 nmol per mouse; i.p.) reaches effective systemic levels, displays a short half-life in the serum and forms an adduct to mmSTING in wild-type mice. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.58 ml | 17.9 ml | 35.799 ml |
5 mM | 0.716 ml | 3.58 ml | 7.16 ml |
10 mM | 0.358 ml | 1.79 ml | 3.58 ml |
5 mM | 0.072 ml | 0.358 ml | 0.716 ml |