2. Immunology/Inflammation NF-κB Cytoskeleton TGF-beta/Smad MAPK/ERK Pathway Metabolic Enzyme/Protease
  3. MyD88 Toll-like Receptor (TLR) NF-κB Collagen TGF-β Receptor p38 MAPK Reactive Oxygen Species (ROS)
  4. LM9

LM9 is a potent, orally active MyD88 inhibitor. LM9 blocks TLR4/MyD88 binding, MyD88 homodimer formation, and TLR4/MyD88/NF-κB signaling pathway activation. LM9 prevents atherosclerosis by regulating inflammatory responses and oxidative stress in macrophages. LM9 efficiently mitigates inflammatory responses and fibrosis in obesity-induced cardiomyopathy. LM9 can be used for fibrosis and atherosclerosis research.

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

LM9

LM9 Chemical Structure

CAS No. : 2249864-11-5

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LM9 Related Antibodies

Top Publications Citing Use of Products

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

  • Biological Activity

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Description

LM9 is a potent, orally active MyD88 inhibitor. LM9 blocks TLR4/MyD88 binding, MyD88 homodimer formation, and TLR4/MyD88/NF-κB signaling pathway activation. LM9 prevents atherosclerosis by regulating inflammatory responses and oxidative stress in macrophages. LM9 efficiently mitigates inflammatory responses and fibrosis in obesity-induced cardiomyopathy. LM9 can be used for fibrosis and atherosclerosis research[1][2].

IC50 & Target[1][2]

NF-κB

 

TLR4

 

Collagen I

 

Collagen IV

 

In Vitro

LM9 (5-10 μM; 1 h pretreat) attenuates Palmitic Acid (PA) (HY-N0830)-induced inflammation in mouse peritoneal macrophages by reducing proinflammatory cytokine production and ICAM-1 expression[1].
LM9 (5-10 μM; 1 h pretreat) suppresses PA-induced inflammation and NF-κB signaling activation in H9C2 cells[1].
LM9 (5-10 μM) inhibits PA-induced TLR4/MyD88 binding and MyD88 homodimer formation in HEK293T cells[1].
LM9 (5-10 μM; 1 h pretreat) alleviates PA-induced lipid accumulation and fibrosis in H9C2 cells, decreasing collagen 1/4 and TGF-β expression[1].
LM9 (24 h) does not affect the viability of mouse primary peritoneal macrophages up to 20 μM[2].
LM9 (10-20 μM; 1 h pretreat) reduces inflammatory responses in mouse primary peritoneal macrophages and RAW264.7 cells exposed to ox-LDL (HY-NP013) by suppressing TLR4-MyD88 complex formation, NF-κB activation, and MAPK phosphorylation[2].
LM9 (10-20 μM; 1 h pretreat) suppresses ox-LDL uptake and foam cell formation in mouse primary peritoneal macrophages, which is associated with reduced CD36 expression[2].
LM9 (10-20 μM; 1 h pretreat) reduces ox-LDL-induced ROS production in mouse primary peritoneal macrophages, and this effect is mediated by MyD88 inhibition[2].

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

LM9 Related Antibodies

Real Time qPCR[1]

Cell Line: H9C2 cells
Concentration: 5; 10 μM
Incubation Time: 1 h pretreat + 12 h with PA
Result: Significantly reduced the mRNA levels of TNF-α, IL-6, ICAM-1, and BNP.
Markly decreased the protein levels of
collagen 1/4 and TGF-β.

ELISA Assay[1]

Cell Line: mouse peritoneal macrophages
Concentration: 5; 10 μM
Incubation Time: 1 h + 24 h with PA
Result: Reduced PA-induced TNF-α, IL-6, and IL-
1β in mouse peritoneal macrophages.
Exhibited a dose-dependent inhibitory effect on the mRNA levels of proinflammatory gene.

Western Blot Analysis[1]

Cell Line: H9C2 cells
Concentration: 5; 10 μM
Incubation Time: 1 h
Result: Markly inhibited the degradation and phosphorylation of IκB-α.
Decreased the accumulation of NF-κB p65 in the nucleus.
Markly decreased the protein levels of
collagen 1/4 and TGF-β.

Western Blot Analysis[2]

Cell Line: RAW264.7 cells; mouse primary peritoneal macrophages
Concentration: 10; 20 μM
Incubation Time: 1 h
Result: Inhibited ox-LDL-induced TLR4-MyD88 complex formation.
Inhibited oxLDL-induced activation of MAPKs.

Immunofluorescence[2]

Cell Line: RAW264.7 cells
Concentration: 10; 20 μM
Incubation Time: 1 h
Result: Decreased the accumulation of NF-κB p65 in the nucleus.
In Vivo

LM9 (5 and 10 mg/kg; i.g.; every 2 days for 8 weeks) mitigates myocardial inflammation, ameliorates fibrosis, improves cardiac function, and normalizes blood lipid profiles in high-fat diet (HFD) mice[1].
LM9 (10 mg/kg; i.g.; every 2 days for 8 weeks) attenuates atherosclerosis in HFD ApoE-/- mice[2].

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

Animal Model: Male C57BL/6J mice (18-22 g) fed with HFD for 16 weeks[1]
Dosage: 5, 10 mg/kg
Administration: i.g.; every 2 days; 8 weeks
Result: Dose-dependently decreased serum CK-MB, CK, triglyceride, total cholesterol, and LDL levels.
Increased HDL levels.
Improved cardiac function indicators (EF%, FS%).
Reduced myocardial TNF-α accumulation, neutrophil infiltration, and mRNA levels of proinflammatory genes (TNF-α, IL-6, ICAM-1).
Decreased collagen deposition and mRNA/protein levels of profibrotic genes (collagen I, collagen IV, TGF-β, BNP).
Inhibited HFD-induced IκB-α degradation.
Animal Model: Male ApoE-/- mice (8-week-old) fed with HFD for 16 weeks[2]
Dosage: 10 mg/kg
Administration: i.g.; every 2 days for 8 weeks
Result: Reduced whole aorta plaque area, aortic root lesion area, α-SMA-positive area, collagen deposition.
Reduced serum TNF-α and IL-6 levels, aortic mRNA levels of IL-1β, TNF-α, IL-6, ICAM, and VCAM, CD68-positive macrophage infiltration.
Reduced CD36 expression (mRNA and protein in aortas), and DHE-positive ROS levels in aortas.
Did not alter body weight or serum lipid levels (TG, TCH, LDL, HDL).
Molecular Weight

497.57

Formula

C24H27N5O5S
CAS No.
SMILES

O=C(CCN1CCN(CC1)CC2=CC([N+]([O-])=O)=CC=C2)NC3=NC(C4=CC(OC)=C(O)C=C4)=CS3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LM9 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LM92249864-11-5LM 9LM-9MyD88Toll-like Receptor (TLR)NF-κBCollagenTGF-β Receptorp38 MAPKReactive Oxygen Species (ROS)Nuclear factor-κBNuclear factor-kappaBTransforming growth factor beta receptorsMyD88 homodimer formationmacrophagesatherosclerosisox-LDLTLR4/MyD88/NF-κB signaling pathwayTLR4/MyD88 bindingobesity-induced cardiomyopathycardiac cellshigh-fat diet-fed miceInhibitorinhibitorinhibit

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