2. Epigenetics
  3. DNA Methyltransferase
  4. 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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DNMT-IN-5 Chemical Structure

DNMT-IN-5 Chemical Structure

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DNMT-IN-5 Related Antibodies

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Description

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[1].

In Vitro

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; 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.

DNMT-IN-5 Related Antibodies

Cell Viability Assay[1]

Cell Line: HCT-116
Concentration: 0.1 μM; 1 μM; 10 μM; 100 μM
Incubation Time: 3 days
Result: Showed very similar cytotoxicity (IC50 = 9.15 μM) among themselves and reference compound MLo1506 (IC50 = 8.18 μM).

RT-PCR[1]

Cell Line: HCT-116
Concentration: 5 μM
Incubation Time: 0 d; 2 d; 5d
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.

Cell Cycle Analysis[1]

Cell Line: HCT-116, DU-145, U2OS
Concentration: 5 μM
Incubation Time: 5 days
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.
Molecular Weight

367.62

Formula

C16H12BrClO3
SMILES

O=C1C(Cl)(C(OC)(OC2=CC=CC=C21)C3=CC=CC=C3)Br
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DNMT-IN-5 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DNMT-IN-5DNA MethyltransferaseDNMTsDNA MTasesInhibitorinhibitorinhibit

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