1. Metabolic Enzyme/Protease
  2. E1/E2/E3 Enzyme
  3. LS-102

LS-102 

Cat. No.: HY-135844 Purity: 96.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

LS-102 Chemical Structure

LS-102 Chemical Structure

CAS No. : 1456891-34-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 132 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
50 mg USD 550 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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 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].

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

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].

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

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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 31.25 mg/mL (69.05 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2095 mL 11.0473 mL 22.0946 mL
5 mM 0.4419 mL 2.2095 mL 4.4189 mL
10 mM 0.2209 mL 1.1047 mL 2.2095 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.60 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.60 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.60 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
LS-102
Cat. No.:
HY-135844
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