2. Epigenetics
  3. Histone Methyltransferase
  4. UNC10013

UNC10013 is an inhibitor targeting the triple Tudor domain (3TD) of SETDB1. UNC10013 covalently binds to Cys385 of SETDB1 3TD, acts as a negative allosteric modulator of the methyltransferase domain of SETDB1, reduces the level of Akt methylation mediated by SETDB1, and blocks Tyr308 phosphorylation of Akt. UNC10013 is applicable to cancer-related research.

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UNC10013

UNC10013 Chemical Structure

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Based on 1 publication(s) in Google Scholar

UNC10013 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 ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

UNC10013 is an inhibitor targeting the triple Tudor domain (3TD) of SETDB1. UNC10013 covalently binds to Cys385 of SETDB1 3TD, acts as a negative allosteric modulator of the methyltransferase domain of SETDB1, reduces the level of Akt methylation mediated by SETDB1, and blocks Tyr308 phosphorylation of Akt. UNC10013 is applicable to cancer-related research[1].

In Vitro

UNC10013 (0.057 μM; 1 h) potently displaces the H3K9Me2K14Ac peptide from wild-type SETDB1 3TD with an IC50 of 0.057 μM[1].
UNC10013 (8.2 μM; 1 h) has reduced potency displacing the H3K9Me2K14Ac peptide from SETDB1 3TDC385A, with an IC50 of 8.2 μM[1].
UNC10013 (12.5-200 nM; 20 min) shows potent targeted covalent reactivity toward SETDB1 3TD, with a kinact/KI ratio of 1.04 × 106 M-1 s-1, a kinact of 6.22 × 10-2 s-1, and a KI of 60 nM[1].
UNC10013 (0.07 μM; 1 h pre-incubation at room temperature) potently displaces the FITC-H3K9Me2K14Ac peptide from SETDB1 3TD with an IC50 of 0.07 μM[1].
UNC10013 (0.027 μM; 1 h) potently displaces the H3K9Me2K14Ac-modified nucleosome from SETDB1 3TD with an IC50 of 0.027 μM[1].
UNC10013 (dose-response curve concentrations) inhibits SETD2 and PRMT1 methyltransferase activities with IC50 values of 0.8 ± 0.1 μM and 1.3 ± 0.1 μM, respectively[1].
UNC10013 (10 μM; 1 h) shows high proteome-wide selectivity, covalently modifying only SETDB1 Cys385 and NCK2 Cys144 when incubated with MCF-7 cell lysate[1].
UNC10013 (10-40 μM; 24 h pretreatment) acts as a negative allosteric modulator of SETDB1, inhibiting SETDB1-mediated Akt methylation and subsequent Akt Tyr308 phosphorylation in HeLa cells at concentrations of 30 μM and above[1].

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

UNC10013 Related Antibodies
Molecular Weight

982.85

Formula

C37H54F12N8O9
Appearance

Oil

Color

Colorless to light yellow

SMILES

O=C(NC1=CC2=C(NCCCCCCN(C)C)N=C(NCCCCCN(C)C)N=C2C=C1)/C=C/CN(C)C.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (101.74 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 1.0174 mL 5.0872 mL 10.1745 mL
5 mM 0.2035 mL 1.0174 mL 2.0349 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 (sealed storage, away from moisture). 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 (sealed storage, away from moisture). 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 1.0174 mL 5.0872 mL 10.1745 mL 25.4362 mL
5 mM 0.2035 mL 1.0174 mL 2.0349 mL 5.0872 mL
10 mM 0.1017 mL 0.5087 mL 1.0174 mL 2.5436 mL
15 mM 0.0678 mL 0.3391 mL 0.6783 mL 1.6957 mL
20 mM 0.0509 mL 0.2544 mL 0.5087 mL 1.2718 mL
25 mM 0.0407 mL 0.2035 mL 0.4070 mL 1.0174 mL
30 mM 0.0339 mL 0.1696 mL 0.3391 mL 0.8479 mL
40 mM 0.0254 mL 0.1272 mL 0.2544 mL 0.6359 mL
50 mM 0.0203 mL 0.1017 mL 0.2035 mL 0.5087 mL
60 mM 0.0170 mL 0.0848 mL 0.1696 mL 0.4239 mL
80 mM 0.0127 mL 0.0636 mL 0.1272 mL 0.3180 mL
100 mM 0.0102 mL 0.0509 mL 0.1017 mL 0.2544 mL
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UNC10013 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:

UNC10013UNC 10013UNC-10013Histone MethyltransferaseSETDB1 methyltransferase domainNCK2PRMT1H3K9Me2K14Ac-modified nucleosomesHeLa cellsMCF-7HEK293T cellsAktSETDB1 triple Tudor domainSETD2Inhibitorinhibitorinhibit

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