L48H37

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 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. (In Vitro):L48H37 inhibits LPS-induced inflammation, particularly TNF-α and IL-6 production and gene expression in mouse macrophages .L48H37 (0-20 μM; 24 hours) decreases the viability of A549 and H460 cells with IC 50 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 IC 50 of 21 μM .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 .L48H37 (4 μM; 16 hours) rapidly induces intracellular ROS levels dose-dependently as detected by increased DCF levels in H460 and A549 cells . Cell Viability Assay Cell Line: A549 and H460 cells; BEAS-2B cells Concentration: 0.625, 1.25, 2.5, 5, 7.5, 10, and 20μM Incubation Time: 24 hours Result: Inhibited lung cancer cells growth in a concentration-dependent manner. Western Blot Analysis Cell Line: A549 and H460 cells Concentration: 0.625, 1.25, 2.5, 5, 7.5, 10, and 20μM 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 . Animal Model: 5‐week‐old athymic BALB/cA nu/nu female mice (18‐22 g) 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.

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Others

Other Targets

NO Synthase;TNF-α;NOS;inflammation;CCL4;Antioxidant

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343307-76-6

483.6

C27H33NO7

>98% (HPLC)

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CCN1CC(=CC2=CC(OC)=C(OC)C(OC)=C2)C(=O)C(C1)=CC1=CC(OC)=C(OC)C(OC)=C1

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(-20℃)

With Ice Pack

≥ 2 years