1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. L48H37

L48H37 

Cat. No.: HY-126154
Handling Instructions

L48H37 is an analog of Curcumin (HY-N0005) with improved chemical stability. L48H37 is a potent and specific myeloid differentiation protein 2 (MD2) inhibitor and inhibits the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 is used for the research of sepsis or lung injury treatment.

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

L48H37 Chemical Structure

L48H37 Chemical Structure

CAS No. : 343307-76-6

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Description

L48H37 is an analog of Curcumin (HY-N0005) with improved chemical stability. L48H37 is a potent and specific myeloid differentiation protein 2 (MD2) inhibitor and inhibits the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 is used for the research of sepsis or lung injury treatment[1].

IC50 & Target[1]

TLR4

 

In Vitro

L48H37 inhibits LPS-induced inflammation, particularly TNF-α and IL-6 production and gene expression in mouse macrophages[1].
L48H37 (0-20 µM; 24 hours) decreases the viability of A549 and H460 cells with IC50 values of 5.3 µM and 2.3 µM, respectively, which is more effective compared to curcumin in lung cancer cells. It shows a low cytotoxicity on normal human lung epithelial cells (BEAS-2B) with IC50 of 21 μM[2].
L48H37 (1, 2, or 4 µM; 16 hours) dose‐dependently inhibited the expression of p‐Cdc2 and Cdc2, and increases the expression of p53. It also shows increased levels of cleaved poly (ADP‐ribosyl) polymerase (PARP) and reduced levels of anti‐apoptotic protein Bcl‐2 in H460 and A549 cells[2].
L48H37 (4 µM; 16 hours) rapidly induces intracellular ROS levels dose-dependently as detected by increased DCF levels in H460 and A549 cells[2].

Cell Viability Assay[2]

Cell Line: A549 and H460 cells; BEAS-2B cells
Concentration: 0.625, 1.25, 2.5, 5, 7.5, 10, and 20 µM
Incubation Time: 24 hours
Result: Inhibited lung cancer cells growth in a concentration-dependent manner.

Western Blot Analysis[2]

Cell Line: A549 and H460 cells
Concentration: 0.625, 1.25, 2.5, 5, 7.5, 10, and 20 µM
Incubation Time: 24 hours
Result: Decreased p‐Cdc2, Cdc2, and Bcl‐2 expression in 2 lung cancer cells.
In Vivo

L48H37 (intraperitoneal injection; 5 mg or 10 mg/kg; once daily; 11‐day ) inhibits H460 xenograft tumor growth and exhibits anti‐tumor activity in mice[1].

Animal Model: 5‐week‐old athymic BALB/cA nu/nu female mice (18‐22 g)[2]
Dosage: 5 mg or 10 mg/kg
Administration: Intraperitoneal injection; once daily; 11‐day
Result: Reduced tumor wet weights as compared to vehicle control.
Decreased the levels of p‐STAT3, and increased the levels of p‐EIF2α and ATF4 in vivo.
Exhibited no significant structural changes in mice.
Molecular Weight

483.55

Formula

C₂₇H₃₃NO₇

CAS No.

343307-76-6

SMILES

O=C1/C(CN(C/C1=C\C2=CC(OC)=C(C(OC)=C2)OC)CC)=C/C3=CC(OC)=C(C(OC)=C3)OC

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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Keywords:

L48H37Toll-like Receptor (TLR)InflammationAsthmalung injurySepsisTLR4/MD2IL-6TNF-αCurcuminInhibitorinhibitorinhibit

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