Dot1L-IN-2 

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

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

Dot1L-IN-2 is a potent, selective Dot1L inhibitor, with an IC₅₀ and K_i 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

476.53

C₂₇H₂₄N₈O

1940206-71-2

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

Room temperature in continental US; may vary elsewhere.

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

• [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.  [Content Brief]