DNMT-IN-5
DNMT-IN-5 is a stable and efficient DNA methyltransferase (DNMT) inhibitor with high stability and high activity with an IC50 of 0.78 nM. DNMT-IN-5 exhibits sub-micromolar DNMT3A inhibitory activity, upregulates the expression of DNMT-targeted genes, impairs cell proliferation, and triggers a critical cell cycle arrest. DNMT-IN-5 can be used for the study of p53-depleted colorectal cancer.
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- CAS No.: 3126555-64-1
- Formule: C16H12BrClO3
- Masse moléculaire:367.62
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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DNMT3A 9.15 μM (IC50) |
DNMT-IN-5 (compound 34b) (0.1-30 μM; 3 days) still exhibits the activity of a DNMT 3A inhibitor at the nanomolar level, with an IC50 value of 9.15 μM in HCT-116 cells[1].
DNMT-IN-5 (5 μM; 0-5 days) significantly induces the upregulation of p15 and p16 expression by 1.76 (88%)-fold and 1.34 (67%)-fold, respectively in HCT-116 cells[1].
DNMT-IN-5 (5 μM; 5 days) on DNMT-regulated genes varies by cell type and is most pronounced in HCT-116 cells[1].
DNMT-IN-5 (5 μM; 5 days) triggers a critical cell cycle arrest in the G1/S transition, notably in p53-depleted HCT-116 colorectal cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116
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Concentration:0.1 μM; 1 μM; 10 μM; 100 μM
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Incubation Time:3 days
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Result:Showed very similar cytotoxicity (IC50 = 9.15 μM) among themselves and reference compound MLo1506 (IC50 = 8.18 μM).
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Cell Line:HCT-116
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Concentration:5 μM
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Incubation Time:0 d; 2 d; 5d
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Result:Significantly induced the upregulation of p15 expression by 1.76 (88%)-fold, compared to nontreated cells.
Increased p16 expression by 1.34 (67%)-fold.
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Cell Line:HCT-116, DU-145, U2OS
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Concentration:5 μM
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Incubation Time:5 days
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Result:Did not alter p15 expression in p53-KO cells but successfully induced p16 re-expression.
Strongly impaired the G1/S transition in the absence of p53 and led to a substantial population of defective replicating cells.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 3126555-64-1
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Masse moléculaire 367.62
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Formule C16H12BrClO3
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SMILES
CO[C@]1(C2=CC=CC=C2)OC3=CC=CC=C3C([C@@]1(Cl)Br)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DNMT-IN-5 Related Classifications
HY-176230 Related Classifications
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