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Chemical Structure| 1456891-34-1 Chemical Structure| 1456891-34-1

Structure of LS-102
CAS No.: 1456891-34-1

Chemical Structure| 1456891-34-1

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

4.5 *For Research Use Only! Not for Human Use. We Do Not Sell to Patients.

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Product Citations

Product Citations

Luo, Hongliang ; Jin, Xiaorui ; Gao, Chengchang ; Deng, Qinqin ; Han, Linfen ; Hu, Fumin , et al.

Abstract: Natural products have emerged as promising therapeutic agents for targeting redox vulnerabilities in cancer. , a bioactive polyphenol derived from philippinensis, exhibits broad anticancer properties through and induction. However, its capacity to modulate , a druggable form of iron-dependent cell death, remains unexplored in hepatocellular carcinoma (HCC). Here, we demonstrate that potently inhibits HCC proliferation by triggering execution, as evidenced by lipid peroxidation accumulation and inhibitor (ferrostatin-1)-rescued cell death. Strikingly, subtherapeutic doses of enhanced the efficacy of clinical inducers (RSL3 and sorafenib), and this chemosensitization effect persisted in PKCδ-depleted models, indicating a target-agnostic mechanism. Mechanistically, orchestrates ubiquitin-proteasomal degradation of two central defense nodes: the transporter SLC7A11 and glutathione peroxidase 4 (GPX4), thereby compromising cellular capacity. This dual-degradation strategy distinguishes from single-target phytochemicals and underlies its robust induction. Our work provides the first demonstration of rottlerin’s ferroptotic activity in HCC, positioning it as a dual degrader capable of overcoming compensatory adaptations. These findings advocate for rottlerin’s clinical development either as monotherapy or in rational combinations to augment ferroptosis-targeted HCC treatment.

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Product Details of LS-102

CAS No. :1456891-34-1
Formula : C24H36N8O
M.W : 452.60
SMILES Code : CCNCCN(CC)C1=NC(NC2=CC=C3N=COC3=C2)=NC(N[C@H](C4CCCCC4)C)=N1
English Name :(S)-N2-(Benzo[d]oxazol-6-yl)-N4-(1-cyclohexylethyl)-N6-ethyl-N6-(2-(ethylamino)ethyl)-1,3,5-triazine-2,4,6-triamine
MDL No. :MFCD32671959
InChI Key :DEDHMXBDEJSZFE-KRWDZBQOSA-N
Pubchem ID :118518043

Safety of LS-102

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Adipose stem cells (HFD-ASCs) 10 µg/mL, 20 µg/mL, 30 µg/mL, 40 µg/mL 6 hours, 12 hours, 24 hours, 48 hours LS-102 significantly inhibited the secretion of TNF-α and PAI-1 by adipose stem cells in a concentration-dependent manner (P < 0.05). Drug Des Devel Ther. 2022 Mar 14;16:647-664
Adipose stem cells (ND-ASCs) 10 µg/mL, 20 µg/mL, 30 µg/mL, 40 µg/mL 6 hours, 12 hours, 24 hours, 48 hours LS-102 significantly inhibited the secretion of TNF-α and PAI-1 by adipose stem cells in a concentration-dependent manner (P < 0.05). Drug Des Devel Ther. 2022 Mar 14;16:647-664
H9c2 cells 0.3125, 0.625, 1.25 µM 24 hours To investigate the protective effect of LS-102 on H9c2 cells against hypoxia/reoxygenation (H/R) injury. Results showed that LS-102 significantly increased cell viability, reduced apoptosis, decreased levels of ROS, CK, LDH, and calcium, and upregulated mitochondrial membrane potential (MMP) and Bax/Bcl-2 ratio. Front Pharmacol. 2020 Sep 17;11:1083

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice C57BL/6J mice Intraperitoneal injection 50 mg/kg Once daily for 2 months To evaluate the effect of LS-102 on weight gain and white adipose tissue accumulation EMBO J. 2015 Apr 15;34(8):1042-55
AG6 mice DENV2 infection model Intraperitoneal injection 15 mg/kg Daily for 7 days Evaluate the effect of LS-102 on DENV2 infection Proc Natl Acad Sci U S A. 2024 Apr 16;121(16):e2317978121
C57BL/6J mice High-fat diet-induced obesity-related nephropathy model Intragastric administration 10 mg/kg, 40 mg/kg Once daily for 4 weeks LS-102 significantly improved perirenal adipose tissue inflammation and renal pathological changes in obesity-related nephropathy model mice and inhibited the TGF-β1/Smad signaling cascade. Drug Des Devel Ther. 2022 Mar 14;16:647-664
Sprague-Dawley rats Myocardial ischemia/reperfusion (I/R) injury model Oral 2.5, 5, 10 mg/kg Single administration, lasting 30 min ischemia and 90 min reperfusion To evaluate the protective effect of LS-102 on myocardial I/R injury in rats. Results showed that LS-102 significantly reduced myocardial infarct size, decreased serum CK-MB and LDH activities, improved ECG parameters and hemodynamics, and reduced the incidence of arrhythmia. Front Pharmacol. 2020 Sep 17;11:1083
Zebrafish embryos Zebrafish embryo model Administration in water 27.8, 83.3, 250 µg/ml 24 hours LS-102 significantly ameliorated astemizole-induced heart rate slowing, increased SV-BA spacing, and prevented arachidonic acid-induced thrombosis in zebrafish Front Pharmacol. 2022 Sep 23;13:987882

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.05mL

2.21mL

1.10mL

22.09mL

4.42mL

2.21mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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