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DNMT1-IN-5

DNMT1-IN-5 (Compound 55) is the inhibitor for DNMT that inhibits DNMT1 and DNMT3A with IC50 of 2.42 μM and 14.4 μM. DNMT1-IN-5 exhibits antiproliferative activity in a variety of cancer cell lines (IC50s for TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226 and HCT116 are 0.19-2.37 μM), arrests the cell cycle at G2/M phase, and induces apoptosis in TMD-8 and DOHH2 cells. DNMT1-IN-5 exhibits antitumor efficacy in TMD-8 xenograft mouse models[1].

Product Specifications

CAS Number

[2982511-19-1]

UNSPSC

12352005

Target

Apoptosis; DNA Methyltransferase

Related Pathways

Apoptosis; Epigenetics

Field of Research

Cancer

Smiles

CN1CCC(NC2=C3C(N(C=C3)CCCN4CCCC4)=NC(C5=CC=NC(F)=C5)=N2)CC1

Molecular Formula

C24H32FN7

Molecular Weight

437.56

References & Citations

[1]Yang L, et al., Design and Synthesis of Novel Deazapurine DNMT 1 Inhibitors with In Vivo Efficacy in DLBCL. J Med Chem. 2025 Mar 13;68 (5) :5333-5357.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

DNMT1; DNMT3

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