1940206-71-2

1940206-71-2 structure

1940206-71-2 structure

Name: Dot1L-IN-2
Chemical Name: Dot1L-IN-2
CAS Number: 1940206-71-2
Molecular Formula: C₂₇H₂₄N₈O
Molecular Weight: 476.53
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2019-02-09 08:38:28
Modify Date: 2024-01-15 11:18:17
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.

Name	Dot1L-IN-2

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	Signaling Pathways >> Epigenetics >> Histone Methyltransferase Research Areas >> Others
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.

Molecular Formula	C₂₇H₂₄N₈O
Molecular Weight	476.53