2. Epigenetics
  3. Histone Methyltransferase
  4. Dot1L-IN-5

Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 0.17 nM.

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

Dot1L-IN-5 Chemical Structure

Dot1L-IN-5 Chemical Structure

CAS No. : 2565705-03-3

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 440 In-stock
Solid
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10 mg USD 680 In-stock
25 mg USD 1350 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Dot1L-IN-5 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-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 0.17 nM[1].

IC50 & Target[1]

DOT1L

0.17 nM (IC50)

In Vitro

Dot1L-IN-5 (Compound 11) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED50 H3K79me2 Elisa=2.9 nM) and HOXA9 gene expression in Molm-13 cells (ED50 HOXA9 RGA=30 nM)[1].

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

Dot1L-IN-5 Related Antibodies
In Vivo

Dot1L-IN-5 (Compound 11; subcutaneous injection; at 75 mg/kg once daily for 20 days) does not lead to tumor growth inhibition in NOD-SCID mice. Dot1L-IN-5 (subcutaneous injection; at 75 mg/kg twice daily for 20 days) leads 73% growth inhibition[1].
While both treatment regimens result in very strong inhibition of global H3K79 dimethylation level in tumor, the efficacious regimen is superior in reducing the mRNA expression of the target genes HOXA9 and MEIS1[1].

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

Animal Model: NOD-SCID mice bearing subcutaneous MV4-11 tumor xenografts[1]
Dosage: 75 mg/kg
Administration: Subcutaneous injection; at 75 mg/kg once or twice daily for 20 days
Result: Once daily administration did not lead to tumor growth inhibition, 73% growth inhibition was measured in the twice daily treated group.
Molecular Weight

592.96

Formula

C23H19ClF2N8O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(N[C@H](C2=NC=CC=C2Cl)C3=C4OC(F)(F)OC4=CC=C3)C(NC5=NC(N)=NC(OC)=N5)=C1)(N)=O
Shipping

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

DMSO : 250 mg/mL (421.61 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 1.6865 mL 8.4323 mL 16.8645 mL
5 mM 0.3373 mL 1.6865 mL 3.3729 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.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C1

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C2

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V2

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

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g

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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 1.6865 mL 8.4323 mL 16.8645 mL 42.1614 mL
5 mM 0.3373 mL 1.6865 mL 3.3729 mL 8.4323 mL
10 mM 0.1686 mL 0.8432 mL 1.6865 mL 4.2161 mL
15 mM 0.1124 mL 0.5622 mL 1.1243 mL 2.8108 mL
20 mM 0.0843 mL 0.4216 mL 0.8432 mL 2.1081 mL
25 mM 0.0675 mL 0.3373 mL 0.6746 mL 1.6865 mL
30 mM 0.0562 mL 0.2811 mL 0.5622 mL 1.4054 mL
40 mM 0.0422 mL 0.2108 mL 0.4216 mL 1.0540 mL
50 mM 0.0337 mL 0.1686 mL 0.3373 mL 0.8432 mL
60 mM 0.0281 mL 0.1405 mL 0.2811 mL 0.7027 mL
80 mM 0.0211 mL 0.1054 mL 0.2108 mL 0.5270 mL
100 mM 0.0169 mL 0.0843 mL 0.1686 mL 0.4216 mL
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Dot1L-IN-5 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-52565705-03-3Histone MethyltransferaseDOT1LH3K79lysinehistonemethyltransferaseInhibitorinhibitorinhibit

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