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HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells. HLM006474 reduces E2F4 protein levels in A375 melanoma cells. HLM006474 induces apoptosis of A375 and MDA-MB-231 breast cancer cells. HLM006474 inhibits A375 proliferation and invasion in a three dimensional skin model of A375 invasion. HLM006474 also attenuates human embryonic stem cell proliferation.
HLM006474 reduces the viability of both SCLC and NSCLC lines with a biological IC50 that varies between 15 and 75 mM, but with no significant difference between the groups. HLM006474 leads to a decrease in the mRNA levels of MAD2. Furthmore, HLM006474 apparently suppresses the increase of Mad2 protein and pRb-S780 signal but not the level of Skp2 protein in human lung cancer A549 cells.
In vivo, HLM006474 leads to significant downregulation of E2F4 protein. Short exposure of Chx10Cre;Rbf/f;p107−/− embryos to HLM006474 has a dramatic effect on tumorigenesis.
| Molecular Weight | 399.48 |
| Formula | C25H25N3O2 |
| CAS Number | 353519-63-8 |
| 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 |
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Products are for research use only. Not for human use. We do not sell to patients.
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