ST-2825

Research use only, not for human use.

A synthetic peptido-mimetic compound that inhibits MyD88 dimerization in a TIR-dependent manner.

A synthetic peptido-mimetic compound that inhibits MyD88 dimerization in a TIR-dependent manner; interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1beta-mediated activation of NF-kappaB transcriptional activity; inhibits IL-1beta-induced production of IL-6 in treated mice, suppresses B cell proliferation and differentiation into plasma cells in response to CpG-induced activation of TLR9; orally active.

ST2825 blocks IL-1R/TLR signaling by interfering with MyD88 homodimerization. ST2825 inhibits this interaction in a concentration-dependent manner with ~40% inhibition of dimerization at 5 μM ST2825 and 80% inhibition at 10 μM ST2825.

ST2825 dose-dependently inhibits IL-1β-induced production of IL-6 in treated mice after oral administration. The animals are administered orally with the appropriate vehicles or ST2825 at doses ranging from 50 to 200 mg/kg, 5 min prior to i.p. injection with 20 μg/kg IL-1β. ST2825 exertes a significant inhibition of IL-1β-stimulated production of IL-6 at 100 and 200 mg/kg.

ST 2825 | ST2825

Immunology/Inflammation

MyD88

MyD88

Inflammation/Immunology

——

894787-30-5

591.506

C27H28Cl2N4O5S

>98% (HPLC)

10 mM in DMSO

O=C([C@@H]1N2[C@](C[C@@]3(N(C(CC4=CC=C(NC(COC5=CC=C(Cl)C=C5Cl)=O)C=C4)=O)CCC3)C2=O)([H])SCC1)N

Spiro[pyrrolidine-2,7'(6'H)-[2H]pyrrolo[2,1-b][1,3]thiazine]-4'-carboxamide, 1-[2-[4-[[2-(2,4-dichlorophenoxy)acetyl]amino]phenyl]acetyl]tetrahydro-6'-oxo-, (2R,4'R,8'aR)-

(-20℃)

With Ice Pack

≥ 2 years