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

Dot1L-IN-1 TFA is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 TFA 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.

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

Dot1L-IN-1 TFA Chemical Structure

Dot1L-IN-1 TFA Chemical Structure

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1 mg USD 300 In-stock
5 mg USD 850 In-stock
10 mg USD 1450 In-stock
25 mg USD 2800 In-stock
50 mg USD 4500 In-stock
100 mg USD 7200 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Dot1L-IN-1 TFA:

Dot1L-IN-1 TFA 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 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Dot1L-IN-1 TFA is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 TFA 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

 

In Vitro

Dot1L-IN-1 (analogue 7) TFA 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 TFA Related Antibodies
Molecular Weight

760.23

Formula

C34H37ClF3N9O4S
Appearance

Solid

Color

Off-white to light yellow

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.OC(C(F)(F)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (65.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3154 mL 6.5770 mL 13.1539 mL
5 mM 0.2631 mL 1.3154 mL 2.6308 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3154 mL 6.5770 mL 13.1539 mL 32.8848 mL
5 mM 0.2631 mL 1.3154 mL 2.6308 mL 6.5770 mL
10 mM 0.1315 mL 0.6577 mL 1.3154 mL 3.2885 mL
15 mM 0.0877 mL 0.4385 mL 0.8769 mL 2.1923 mL
20 mM 0.0658 mL 0.3288 mL 0.6577 mL 1.6442 mL
25 mM 0.0526 mL 0.2631 mL 0.5262 mL 1.3154 mL
30 mM 0.0438 mL 0.2192 mL 0.4385 mL 1.0962 mL
40 mM 0.0329 mL 0.1644 mL 0.3288 mL 0.8221 mL
50 mM 0.0263 mL 0.1315 mL 0.2631 mL 0.6577 mL
60 mM 0.0219 mL 0.1096 mL 0.2192 mL 0.5481 mL
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Dot1L-IN-1 TFA Related Classifications

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-1Histone MethyltransferaseDot1LH3K79 dimethylationHoxA9 promoterHeLaMolm-13Inhibitorinhibitorinhibit

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