Home Cell Cycle CDK inhibitor HLM006474 For research use only.

HLM006474

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.

HLM006474 Chemical Structure

HLM006474 Chemical Structure

CAS: 353519-63-8

Selleck's HLM006474 has been cited by 1 publication

Purity & Quality Control

Batch: S896301 DMSO] 10 mg/mL] false] Water] ˂1 mg/mL] false] Ethanol] ˂1 mg/mL] false Purity: 99.57%
99.57

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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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Chx10Cre mice, Rbf/f mice, p107−/− mice
Dosages 100 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 399.48 Formula

C25H25N3O2
CAS No. 353519-63-8 SDF --
Smiles CCOC1=C(C=C(C=C1)C(C2=C(C3=C(C=CC(=N3)C)C=C2)O)NC4=CC=CC=N4)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 10 mg/mL ( (25.03 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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