| Name | E6446 dihydrochloride |
| Description | E6446 dihydrochloride is a novel synthetic antagonist for nucleic acid-sensing TLRs; potently suppressed DNA stimulation of HEK:TLR9 cells with IC50 of 10 nM. |
| In vitro | E6446 potently inhibited IL-6 production induced by CpG2216 but was ineffective against induction by the TLR3 ligand poly inosine-cytosine. E6446 showed a modest but consistent superiority over AT791, and both were significantly more potent than hydroxychloroquine. Significantly, 250 nM and 1.25 μM E6446 completely suppressed all of the CpG oligo-induced changes in gene expression [1]. E6446 specifically inhibited TLR9 activation with CpG ODN 2006, in the range of 0.01–0.03 μM. A 100-fold higher concentration (2–8 μM) of E6446 was required to inhibit TLR7/8 activated by the imidazoquinoline compound R848 [2]. |
| In vivo | To test their activity in vivo, mice were orally dosed with 20 mg/kg of AT791 or E6446 and 18 hours later were challenged with 60 μg CpG1668 oligonucleotide injected subcutaneously. CpG1668-induced IL-6 production was inhibited ~50% by AT791 and almost completely by E6446 [1]. therapy with E6446 diminished the activation of TLR9 and prevented the exacerbated cytokine response observed during acute Plasmodium infection [2]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 5.23 mg/mL (10.01 mM), Sonication is recommended.
|
| Keywords | TLR | E-6446 Dihydrochloride | E6446 dihydrochloride | E-6446 | E6446 | E 6446 Dihydrochloride | E 6446 |
| Inhibitors Related | D-Glucuronic acid | Hydroxychloroquine | Benzyl alcohol | Sesamin | (±)-Naringenin | Chloroquine phosphate | Chloranil | Thiamine hydrochloride | 2,4,5-Trimethoxybenzoic acid | Resiquimod | Stevioside | DHBP |
| Related Compound Libraries | Bioactive Compound Library | Anti-Alzheimer's Disease Compound Library | Membrane Protein-targeted Compound Library | HIF-1 Signaling Pathway Compound Library | Pyroptosis Compound Library | Inhibitor Library | NO PAINS Compound Library | Immuno-Oncology Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Infection Compound Library | Anti-COVID-19 Compound Library |
United States
