2. Epigenetics
  3. Histone Methyltransferase
  4. Dot1L-IN-1

Dot1L-IN-1 is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 potently suppresses H3K79 dimethylation (IC50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Dot1L-IN-1 TFA) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

Dot1L-IN-1 Chemical Structure

Dot1L-IN-1 Chemical Structure

CAS No. : 2088518-50-5

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Other Forms of Dot1L-IN-1:

Dot1L-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

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Description

Dot1L-IN-1 is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 potently suppresses H3K79 dimethylation (IC50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively[1].

IC50 & Target[1]

DOT1L

 

Cellular Effect
Cell Line Type Value Description References
HeLa IC50
3 nM
Compound: 7
Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79me2 level after 72 hrs by ELISA
Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79me2 level after 72 hrs by ELISA
[PMID: 28337327]
MV4-11 IC50
5 nM
Compound: 7
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 treated for 6 hrs measured after 8 days by Celltiter-Glo reagent based assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 treated for 6 hrs measured after 8 days by Celltiter-Glo reagent based assay
[PMID: 28337327]
In Vitro

Dot1L-IN-1 (analogue 7) effectively inhibits proliferation of the human MLL-rearranged leukemia cell line MV4-11 carrying the oncogenic MLL-AF4 fusion (IC50=5 nM)[1].

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

Dot1L-IN-1 Related Antibodies
Molecular Weight

646.21

Formula

C32H36ClN9O2S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Dot1L-IN-1 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dot1L-IN-12088518-50-5Histone MethyltransferaseDot1LH3K79 dimethylationHoxA9 promoterHeLaMolm-13Inhibitorinhibitorinhibit

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