Inflachromene

SKU: orb1703358

Description

Inflachromene (ICM) is a small molecule inhibitor of HMGB1/2 with anti-inflammatory properties. It has been shown to reduce seizure severity in murine epilepsy models and to inhibit endothelial proliferation and autophagy in vitro via HMGB/TLR4-NF-κB and Beclin 1 pathways, making it a useful research tool for neuroinflammation and autophagy studies.

Research Area

Signal Transduction

Key Properties

• CAS Number: 908568-01-4
• MW: 377.39
• Purity: 99.88% (May vary between batches)
• Formula: C₂₁H₁₉N₃O₄
• SMILES: CC1(C)Oc2cc(O)ccc2C2C1=CCn1n2c(=O)n(-c2ccccc2)c1=O
• Target: JNK,Others,ERK,p38 MAPK,NF-κB
• Solubility: DMSO:80 mg/mL (211.98 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (8.74 mM)

Bioactivity

• In Vivo:
  In a dose-dependent manner (2-10 mg/kg; i.p. once daily for 4 days), Inflachromene effectively blocks LPS-mediated microglial activation. For a duration of 30 days (10 mg/kg; i.p. once daily), Inflachromene significantly reduces the progression of disease, as determined by EAE clinical score. When administered intravenously (i.v.) at a dose of 1 mg/kg, Inflachromene exhibits a long half-life (14.1±6.43 h) and moderate Vss (2.02±1.02 L/kg). Given orally (p.o.) at a dose of 1 mg/kg, Inflachromene shows high oral bioavailability (94%) and Cmax (0.59±0.16 g/mL).
  Read more...
• In Vitro:
  In BV-2 microglial cells, Inflachromene efficiently blocks LPS-induced nitrite release in a dose-dependent manner (0.01-100 μM; 24 h) without any toxicity. After LPS stimulation, Inflachromene (1-10 μM) suppresses the increased levels of inflammation-related genes, such as Il6, Il1b, Nos2, and Tnf. At a concentration of 5 μM, Inflachromene reduces LPS-induced secretion of the proinflammatory cytokine TNF-α. In microglia, Inflachromene (5 μM; 30 min) substantially suppresses the nuclear translocation of NF-κB and the degradation of IκB. The phosphorylation of ERK, JNK, and p38 MAPK in microglia induced by LPS is inhibited by Inflachromene (1-10 μM; 30 min). In the co-culture of neuroblastoma and primary neuronal cells, Inflachromene (10 μM; 30 min) completely prevents the death by inhibiting microglia-mediated neurotoxicity.There is no significant effect on the viability of neurons with Inflachromene (1-10 μM; 24 h).
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HMGB, ICM, Inflachromene

Compound Identifiers

PubChem CID

49857340