HLM006474

Catalog No.S8963 Batch:S896301

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Technical Data

Formula

C25H25N3O2
Molecular Weight 399.48 CAS No. 353519-63-8
Solubility (25°C)* In vitro DMSO 10 mg/mL (25.03 mM)
Water ˂1 mg/mL
Ethanol ˂1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description HLM006474 is a small molecule pan-E2F inhibitor that inhibits DNA binding to E2F4 with IC50 of 29.8 µM in A375 cells. HLM006474 induces a reduction in cell proliferation and an increase in apoptosis. The CDK/Rb/E2F pathway is commonly disrupted in lung cancer, and HLM006474 is shown to have efficacy in lung cancer.
Targets
E2F4 [1]
(Cell-free assay)
29.8 μM
In vitro

Treatment of multiple cell lines with HLM006474 results in the loss of intracellular E2F4 DNA-binding activity within hours. Overnight exposure to HLM006474 results in down regulation of total E2F4 protein as well as known E2F targets. The effects of HLM006474 treatment on different cell lines varies, but includes a reduction in cell proliferation and an increase in apoptosis.[1] 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.[2]
In vivo

HLM006474 inhibits E2F4 DNA-binding and activity in vivo. In vivo HLM006474 leads to significant downregulation of E2F4 protein.[1] Short exposure of Chx10Cre;Rbf/f;p107−/− embryos to HLM006474 has a dramatic effect on tumorigenesis. Thus, modest and temporary pharmaceutical E2f inhibition blocks retinoblastoma initiation.[3]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    3T3 MEFS, A375, MDA-MB-231, MCF7, T47D, HFFs, MDA-MB-468, SK-BR3, 8226-s, 8226-dox40, 8226-MR20

  • Concentrations

    0-100 μM

  • Incubation Time

    0-24 h

  • Method

    Human A375 melanocytes are treated for 9-hrs with the indicated concentration of HLM006474. A375 cells are treated with 40 μM HLM006474 and EMSA and Western analyses performs at the indicated time intervals.
Animal Study:

[3]
  • Animal Models

    Chx10Cre mice, Rbf/f mice, p107−/− mice

  • Dosages

    100 mg/kg

  • Administration

    IP

Selleck's HLM006474 has been cited by 1 publication

E2F and STAT3 provide transcriptional synergy for histone variant H2AZ activation to sustain glioblastoma chromatin accessibility and tumorigenicity [ Cell Death Differ, 2022, 10.1038/s41418-021-00926-5] PubMed: 35058574

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.