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

Dot1L-IN-2 

Cat. No.: HY-111390
Handling Instructions

Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively.

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

Dot1L-IN-2 Chemical Structure

Dot1L-IN-2 Chemical Structure

CAS No. : 1940206-71-2

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Description

Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively.

IC50 & Target

IC50: 0.4 nM (Dot1L)[1]
Ki: 0.08 nM (Dot1L)[1]

In Vitro

Dot1L-IN-2 is a potent, selective Dot1L inhibitor, with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively. Dot1L-IN-2 potently inhibits H3K79 dimethylation (IC50, 16 nM), and blocks the activity of the HoxA9 promoter (IC50, 340 nM) in cellular systems. Dot1L-IN-2 also dramatically suppresses proliferation of the human MLL-rearranged leukemia cell line MV4-11 carrying the oncogenic MLL-AF4 fusion (IC50, 128 nM)[1].

Molecular Weight

476.53

Formula

C₂₇H₂₄N₈O

CAS No.

1940206-71-2

SMILES

CN1C=NC2=CC(OC3=CC=CC=C3N4C(C)=CC5=C4C=C(NC6=NC=CC(NC)=N6)C=C5)=CN=C21

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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