| Identification | Back Directory | [Name]
LS-102 | [CAS]
1456891-34-1 | [Synonyms]
LS-102
LS 102,LS102
1,3,5-Triazine-2,4,6-triamine, N4-6-benzoxazolyl-N6-[(1S)-1-cyclohexylethyl]-N2-ethyl-N2-[2-(ethylamino)ethyl]-
(S)-N2-(Benzo[d]oxazol-6-yl)-N4-(1-cyclohexylethyl)-N6-ethyl-N6-(2-(ethylamino)ethyl)-1,3,5-triazine-2,4,6-triamine | [Molecular Formula]
C24H36N8O | [MDL Number]
MFCD32671959 | [MOL File]
1456891-34-1.mol | [Molecular Weight]
452.6 |
| Chemical Properties | Back Directory | [Boiling point ]
633.8±61.0 °C(Predicted) | [density ]
1.208±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
9.60±0.19(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
LS-102 (1.3-4 mg/kg; i.p.; daily for 4 weeks) reduces clinical severity scores in a CIA model[1]. | Animal Model: | 7-week-old DBA/1 male mice (CIA model)[1] | | Dosage: | 1.3, 4.0 mg/kg | | Administration: | I.p.; daily for 4 weeks | | Result: | Reduced the clinical severity scores.
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| [References]
[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. DOI:10.3892/ijmm.2012.1129
[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. DOI:10.3892/mmr.2018.9576 |
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