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Dot1L-IN-1

Dot1L-IN-1 is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of 50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively[1].

Product Specifications

CAS Number

[2088518-50-5]

UNSPSC

12352005

Hazard Statement

H315-H319-H335

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Dot1L-IN-1.html

Solubility

10 mM in DMSO

Smiles

CC1=NC=CC=C1C2=C(Cl)SC3=CC=C(NC(NCC(NCCCN(C)[C@@H]4CCCN(C5=C(C=CN6)C6=NC=N5)C4)=O)=O)C=C32

Molecular Formula

C32H36ClN9O2S

Molecular Weight

646.21

Precautions

P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P362-P403+P233-P405-P501

References & Citations

[1]Möbitz H, et al. Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach. ACS Med Chem Lett. 2017 Feb 14;8 (3) :338-343.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

DOT1L

Curated Selection

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