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LS-102 

目录号: HY-135844
产品使用指南

LS 102是一种选择性的 synoviolin (Syvn1) 抑制剂。LS-102 抑制 Syvn1 自泛素化,IC50 为 15 μM,有治疗类风湿关节炎的潜力。

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LS-102 Chemical Structure

LS-102 Chemical Structure

CAS No. : 1456891-34-1

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Description

LS-102 is a selective synoviolin inhibitor (Syvn1). LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of ~15 μM. LS-102 has the potential for rheumatoid arthritis treatment[1][2].

In Vitro

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].

Cell Viability Assay[1]

Cell Line: Rheumatoid synovial cells (RSCs)
Concentration: 20, 40, 60 μM
Incubation Time: 12 hours
Result: Inhibited proliferation of RSCs with an IC50 of 5.4 µM.
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.
Molecular Weight

452.60

Formula

C₂₄H₃₆N₈O

CAS No.

1456891-34-1

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

LS-102LS102LS 102OthersproliferationrheumatoidsynovialcellsNRF2severityscoresCIAarthritisInhibitorinhibitorinhibit

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产品名称:
LS-102
目录号:
HY-135844
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