LS-102 

LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC₅₀ of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment^[1][2].

LS-102 inhibits proliferation of RSCs with an IC₅₀ of 5.4 μM^[1].
LS-102 suppresses proliferation of rheumatoid synovial cells (RSCs) in a Syvn1-dependent manner. LS-102 suppresses polyubiquitination of target proteins of Syvn1, including nuclear factor erythroid 2-related factor 2 (NRF2), V247M α-sarcoglycan mutant, and PGC-1β. LS-102 inhibits E3 ligase activity of Synoviolin (Syvn1)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LS-102 (1.3-4 mg/kg; i.p.; daily for 4 weeks) reduces clinical severity scores in a CIA model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

452.60

C₂₄H₃₆N₈O

1456891-34-1

Solid

White to light yellow

CCNCCN(CC)C1=NC(NC2=CC=C3N=COC3=C2)=NC(N[C@H](C4CCCCC4)C)=N1

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [1]. Yagishita N, et al. RING-finger type E3 ubiquitin ligase inhibitors as novel candidates for the treatment of rheumatoidarthritis. Int J Mol Med. 2012 Dec;30(6):1281-6.  [Content Brief]

  [2]. Fujita H, et al. Identification of the inhibitory activity of walnut extract on the E3 ligase Syvn1. Mol Med Rep. 2018 Dec;18(6):5701-5708.  [Content Brief]