1. Epigenetics
  2. Histone Methyltransferase
  3. Dot1L-IN-1

Dot1L-IN-1 

Cat. No.: HY-101520
Handling Instructions

Dot1L-IN-1 is a highly potent, selective and structurally novel Dot1L inhibitor with a Ki of 2 pM.

For research use only. We do not sell to patients.

Dot1L-IN-1 Chemical Structure

Dot1L-IN-1 Chemical Structure

CAS No. : 2088518-50-5

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Description

Dot1L-IN-1 is a highly potent, selective and structurally novel Dot1L inhibitor with a Ki of 2 pM.

IC50 & Target

Ki: 2 pM (Dot1L)[1]

In Vitro

Dot1L-IN-1 potently suppresses H3K79 dimethylation (IC50 = 3 nM), the direct product of the Dot1Lcatalyzed reaction, as well as the activity of the HoxA9 promoter (IC50 = 17 nM) in HeLa and Molm-13 cells, respectively[1].

Dot1L-IN-1 effectively inhibits proliferation of the human MLL-rearranged leukemia cell line MV4-11 carrying the oncogenic MLL-AF4 fusion (IC50 = 5 nM)[1].

Molecular Weight

646.21

Formula

C₃₂H₃₆ClN₉O₂S

CAS No.

2088518-50-5

SMILES

CC1=NC=CC=C1C2=C(Cl)SC3=CC=C(NC(NCC(NCCCN(C)[[email protected]@H]4CCCN(C5=C(C=CN6)C6=NC=N5)C4)=O)=O)C=C32

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Dot1L-IN-1
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