1. Epigenetics
  2. Histone Methyltransferase

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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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0985 mL 10.4925 mL 20.9850 mL
5 mM 0.4197 mL 2.0985 mL 4.1970 mL
10 mM 0.2099 mL 1.0493 mL 2.0985 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Dot1L-IN-2
Cat. No.:
HY-111390
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Dot1L-IN-2

Cat. No.: HY-111390