HLM006474

CAS No. 353519-63-8

HLM006474 ( —— )

Catalog No. M22127 CAS No. 353519-63-8

HLM006474 is a pan inhibitor of E2F. This inhibits E2F4 DNA-binding (IC50: 29.8 μM in A375 cells).HLM006474 causes the viability of both SCLC and NSCLC lines (IC50 ranging from 15 to 75 μM). HLM006474 displays little activities against E2F4 DNA-binding in A375 cells at 10 and 20 μM, apparently inhibits E2F4 DNA-binding at 40 μM, and increasingly suppresses the effect at 60 and 80 μM concentrations.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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25MG 149 In Stock
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Biological Information

  • Product Name
    HLM006474
  • Note
    Research use only, not for human use.
  • Brief Description
    HLM006474 is a pan inhibitor of E2F. This inhibits E2F4 DNA-binding (IC50: 29.8 μM in A375 cells).HLM006474 causes the viability of both SCLC and NSCLC lines (IC50 ranging from 15 to 75 μM). HLM006474 displays little activities against E2F4 DNA-binding in A375 cells at 10 and 20 μM, apparently inhibits E2F4 DNA-binding at 40 μM, and increasingly suppresses the effect at 60 and 80 μM concentrations.
  • Description
    HLM006474 is a pan inhibitor of E2F. This inhibits E2F4 DNA-binding (IC50: 29.8 μM in A375 cells).HLM006474 causes the viability of both SCLC and NSCLC lines (IC50 ranging from 15 to 75 μM). HLM006474 displays little activities against E2F4 DNA-binding in A375 cells at 10 and 20 μM, apparently inhibits E2F4 DNA-binding at 40 μM, and increasingly suppresses the effect at 60 and 80 μM concentrations. HLM006474 dramatically causes cyclin D3 protein expression and is a potent inducer of PARP cleavage[1]. HLM006474 (20 μM) weakly synergizes with paclitaxel, but there is antagonism between HLM006474 and cisplatin and gemcitabine in H1299 cells[2]. HLM006474 (40 μM) inhibits E2F4 activity via suppression of its DNA-binding activity and down regulation of its expression and HLM006474 (40 μM) also obviously causes apoptosis in A375 and 231 cell lines for 24 hours. HLM006474 (60 μM) enhances the expression of several known E2F-regulated genes after short treatments in H292 and H1299 cell lines. HLM006474 leads to a reduction in the mRNA levels of MAD2. HLM006474 apparently suppresses the increase of Mad2 protein and pRb-S780 signal but not the level of Skp2 protein in human lung cancer A549 cellss.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    E2F4 DNA-binding
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    353519-63-8
  • Formula Weight
    399.48
  • Molecular Formula
    C25H25N3O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:24 mg/mL (60.08 mM; Need ultrasonic)
  • SMILES
    CCOc1ccc(cc1C)C(Nc1ccccn1)c1ccc2ccc(C)nc2c1O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Ma Y, et al. A small-molecule E2F inhibitor blocks growth in a melanoma culture model. Cancer Res. 2008 Aug 1;68(15):6292-9.2. Kurtyka CA, et al. E2F inhibition synergizes with paclitaxel in lung cancer cell lines. PLoS One. 2014 May 15;9(5):e96357.
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