Home Cell Cycle CDK inhibitor HLM006474

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HLM006474 CDK inhibitor

Cat.No.S8963

HLM006474 is a small molecule pan-E2F inhibitor that inhibits DNA binding to E2F4 with IC50 of 29.8 µM in A375 cells. This compound induces a reduction in cell proliferation and an increase in apoptosis. The CDK/Rb/E2F pathway is commonly disrupted in lung cancer, and this chemical is shown to have efficacy in lung cancer.
HLM006474 CDK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 399.48

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 399.48 Formula

C25H25N3O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 353519-63-8 -- Storage of Stock Solutions

Synonyms N/A Smiles CCOC1=C(C=C(C=C1)C(C2=C(C3=C(C=CC(=N3)C)C=C2)O)NC4=CC=CC=N4)C

Solubility

In vitro
Batch:

DMSO : 10 mg/mL (25.03 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
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 this compound results in down regulation of total E2F4 protein as well as known E2F targets. The effects of this chemical treatment on different cell lines varies, but includes a reduction in cell proliferation and an increase in apoptosis.[1] This compound 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 this compound leads to significant downregulation of E2F4 protein.[1] Short exposure of Chx10Cre;Rbf/f;p107−/− embryos to this chemical has a dramatic effect on tumorigenesis. Thus, modest and temporary pharmaceutical E2f inhibition blocks retinoblastoma initiation.[3]
References

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