An inhibitor of the transcription factor E2F (IC50 = 29.8 µM for E2F4); inhibits DNA binding to E2F1

HLM006474 – 10 mg

Brand:
Cayman
CAS:
353519-63-8
Storage:
-20
UN-No:
Non-Hazardous - /

HLM006474 is a non-selective inhibitor of the transcription factor E2F (IC50 = 29.8 µM for E2F4).{45457} It inhibits DNA binding to E2F1, E2F2, and E2F4 in A375 melanoma cells when used at a concentration of 40 µM. HLM006474 (40 µM) decreases protein levels of E2F4 and cyclin D3 and induces apoptosis in A375 cells. It also induces apoptosis in MDA-MB-231, but not MCF-7, cells and inhibits the growth of cancer cells in a panel of 17 lung cancer cell lines (IC50s = 15.5-75.1 µM).{45457,45458} HLM006474 reduces tumor growth in retinoblastoma-prone Chx10Cre;Rbfl/fl;p107-/- mice and in an A375 mouse xenograft model when administered at a dose of 100 mg/kg and 2 mg per mouse, respectively.{45459,45460}  

 

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SKU: 28276 - 10 mg Category:

Description

An inhibitor of the transcription factor E2F (IC50 = 29.8 µM for E2F4); inhibits DNA binding to E2F1, E2F2, and E2F4 in A375 melanoma cells at 40 µM; decreases protein levels of E2F4 and cyclin D3 and induces apoptosis in A375 cells; induces apoptosis in MDA-MB-231, but not MCF-7, cells at 40 µM and inhibits the growth of cancer cells in a panel of 17 lung cancer cells (IC50s = 15.5-75.1 µM); reduces tumor growth in retinoblastoma-prone Chx10Cre;Rbfl/fl;p107-/- mice and in an A375 mouse xenograft model at 100 mg/kg and 2 mg per mouse, respectively

Formal name: 7-[(4-ethoxy-3-methylphenyl)(2-pyridinylamino)methyl]-2-methyl-8-quinolinol

Synonyms: 

Molecular weight: 399.5

CAS: 353519-63-8

Purity: ≥95%

Formulation: A solid

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