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LY2940680 is a Hedgehog inhibitor in clinical trials. LY2940680 binds to the Smo receptor and potently inhibits Hh signaling. LY2940680 inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib. LY2940680 induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. LY2940680 is currently being tested in phase I trials for people with a range of solid tumors.
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Source | PLoS One (2015). Figure 3. LY2940680 |
| Method | MTS assay | |
| Cell Lines | CCA Cell | |
| Concentrations | 50 μM | |
| Incubation Time | 72 h | |
| Results | In contrast, Vismodegib, a small-molecule antagonist of Smoothened and LY2940680, a small-molecule antagonist of the smoothened receptor, showed a slight inhibitory effect on cell proliferation without differences between mucin-(IC50: Vismodecib = 61.7 ± 1.4 μM, LY2940680 = 49.8 ± 4.5 μM) and mixed-CCA (IC50: Vismodecib = 81.6 ± 14.8 μM, LY2940680 = 61.2 ± 21.1 μM). |
| Molecular Weight | 512.5 |
| Formula | C26H24F4N6O |
| CAS Number | 1258861-20-9 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Hedgehog Products |
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PF-5274857 is a novel Smoothened antagonist, inhibits Hedgehog signaling with IC50 and Ki values of 5.8 nM and 4.6 nM, respectively. |
| Jervine
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| Ciliobrevin A
Ciliobrevin A (HPI-4) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo. |
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