| Name | EC 144 |
| Description | EC 144, a second-generation selective inhibitor of Hsp90 (heat shock protein 90), inhibits tumor growth with an IC50= 1.1 nM for Hsp90α and an EC50 = 14 nM for degradation of Her-2 in MCF-7 cells. |
| In vitro | EC 144 is a synthetic Hsp90 inhibitor, blocks LPS-induced TLR4 signaling in RAW 264.7 cells by inhibiting activation of ERK1/2, MEK1/2, JNK, and p38 MAPK but not NF-κB. EC 144 inhibited CD4(+) T cell proliferation in both mouse and human mixed lymphocyte reactions (MLRs), indicating an immunosuppressive effect on adaptive immune activation. [1] |
| In vivo | In mice treated with EC 144, peritoneal CD11b(+) exudate cells showed reduced phosphorylation of tumor progression locus 2, MEK1/2, and ERK1/2 upon LPS challenge. This corresponded with resistance to LPS-induced systemic inflammation and suppressed TNF-α release. In a mouse collagen-induced arthritis model, EC 144 suppressed arthritis development, correlated with a reduction in antigen-specific antibody production and impaired activation of antigen-specific CD4(+) T cells. [1] |
| Storage | keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.83 mM), Sonication is recommended. DMSO : 50 mg/mL (120.8 mM), Sonication is recommended.
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| Keywords | EC-144 | EC 144 |
| Inhibitors Related | Ethoxyquin | Adezmapimod | Tamoxifen | Palmitic acid sodium | Mequinol | 7-Aminocephalosporanic acid | Benzbromarone | Elesclomol | Rifabutin | Palmitic acid | Tamoxifen Citrate | Isoxazole |