Dot1L-IN-2

Modify Date: 2025-08-27 01:44:28

Dot1L-IN-2 Structure
Dot1L-IN-2 structure
Common Name Dot1L-IN-2
CAS Number 1940206-71-2 Molecular Weight 476.53
Density N/A Boiling Point N/A
Molecular Formula C27H24N8O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Dot1L-IN-2


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.

 Names

Name Dot1L-IN-2

 Dot1L-IN-2 Biological Activity

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.
Related Catalog
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].
References

[1]. Chen C, et al. Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach. ACS Med Chem Lett. 2016 Jun 1;7(8):735-40.

 Chemical & Physical Properties

Molecular Formula C27H24N8O
Molecular Weight 476.53
InChIKey RQVLGMREYUFLPQ-UHFFFAOYSA-N
SMILES CNc1ccnc(Nc2ccc3cc(C)n(-c4ccccc4Oc4cnc5c(c4)ncn5C)c3c2)n1
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