| Bioactivity | LMT-28 is an orally active and the first synthetic IL-6 inhibitor that functions through direct binding to gp130. LMT-28 shows low toxicity and selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130[1]. | ||||||||||||
| Invitro | LMT-28 reduces IL-6-induced luciferase activity by ~90% at a concentration of 50 μM and exhibits an IC50 value of 5.9 μM. LMT-28 (1-10 μM; 72 hours) inhibits IL-6-induced proliferation of the human erythroleukemic cell line TF-1[1].LMT-28 (1-100 μM; 1 hour) selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130[1]. Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| In Vivo | LMT-28 (0-0.5 mg/kg; p.o.; once daily for 15 days) alleviates CIA in mice[1].LMT-28 (0.25 or 1 mg/kg; p.o.) ameliorates the progression of pancreatitis in mice. LMT-28 binds directly and specifically to gp130, and thereby inhibits the interaction of gp130 with the IL-6/IL-6Rα complex[1]. Animal Model: | ||||||||||||
| Name | LMT-28 | ||||||||||||
| CAS | 1239600-18-0 | ||||||||||||
| Formula | C17H29NO4 | ||||||||||||
| Molar Mass | 311.42 | ||||||||||||
| Appearance | Oil | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Hong SS, et al. A Novel Small-Molecule Inhibitor Targeting the IL-6 Receptor β Subunit, Glycoprotein 130. J Immunol. 2015 Jul 1;195(1):237-45. |
LMT-28
CAS: 1239600-18-0 F: C17H29NO4 W: 311.42
LMT-28 is an orally active and the first synthetic IL-6 inhibitor that functions through direct binding to gp130. LMT-28
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