HE 3286 (C09-1138-177)

HE 3286 is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. HE 3286 is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. HE 3286 freely penetrates the blood brain barrier in mice. HE 3286 can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitisIn VitroHE 3286 attenuates NF-κB phosphorylation, but not influences IκB phosphorylation of LPS-induces (100 ng/mL; 0-2 hours) murine macrophages. HE 3286 (100 nM, overnight) partially blocks the activation of IKK, JNK, p38, and ERK of LPS-induces (100 ng/mL; 0-2 hours) murine macrophages. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: LPS-induced murine macrophages Concentration: 100 nM Incubation Time: overnight Result: Attenuated NF-κB phosphorylation. Blocked the activation of IKK, JNK, p38, and ERK partially.In VivoHE 3286 (25-50 mg/kg; oral gavage; daily for 22-49 days) reduces joint inflammation, synovial proliferation, and erosion of DBA/1 Lac male collagen-induced arthritis mice . HE 3286 (40 mg/kg; intraperitoneal injection; daily for 40 days) suppresses inflammation, reduces demyelination and axonal loss, and promotes RGC survival during experimental optic neuritis of experimental autoimmune encephalomyelitis mice. HE 3286 (80 mg/kg; 0-24h) freely penetrates the BBB in male CD-1 mice. HE 3286 (40 mg/kg; gavage; twice-daily for 4 days) increases the numbers of tyrosine hydroxylase-positive cells and decreases the numbers of damaged neurons in Parkinson's disease mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:NF-κB. Specification: ≥95.0% Molecular Formula: C21H30O3 Molecular Weight: 330.46 PubChem CID: 16739648 Isomeric SMILES: C[C@]12CC[C@@H](CC1=C[C@@H]([C@@H]3[C@@H]2CC[C@]4([C@H]3CC[C@]4(C#C)O)C)O)O