2. Epigenetics
  3. Histone Methyltransferase
  4. OTS186935

OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells.

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OTS186935

OTS186935 構造式

CAS 番号 : 2093400-18-9

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 306 在庫あり
Solution
10 mM * 1 mL in DMSO USD 306 在庫あり
Solid
5 mg $300 在庫あり
10 mg $500 在庫あり
25 mg $1000 在庫あり
50 mg $1400 在庫あり
100 mg $1950 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 4 publication(s) in Google Scholar

Other Forms of OTS186935:

OTS186935 関連抗体

Top Publications Citing Use of Products

Histone Methyltransferase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
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

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  • 純度とドキュメンテーション

  • 参考文献

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製品説明

OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells[1].

IC50 & Target

IC50: 6.49 nM (SUV39H2)[1]
体外実験

OTS186935 inhibits A549 cell growth with an IC50 of 0.67 μM[1].

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

OTS186935 関連抗体
体内実験

OTS186935 (10 mg/kg or 25 mg/kg; intravenously; once daily for 14 days) exhibits growth suppressive effects in human cancer cell line derived xenograft models[1].

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

Animal Model: Female NOD.CB17-Prkdcscid/J mice (bearing MDA-MB-231 cells )[1]
Dosage: 10 mg/kg
Administration: Intravenously; once daily for 14 days
Result: Tumor growth inhibition of 42.6% on day 14.
Animal Model: Female BALB/cAJcl-nu/nu mice (bearing A549 cells)[1]
Dosage: 25 mg/kg
Administration: Intravenously; once daily for 14 days
Result: Yielded a tumor growth inhibition of 60.8% without significant body weight loss or toxicity.
分子量

463.96

分子式

C25H26ClN5O2
CAS 番号
Appearance

Solid

Color

Off-white to light yellow

SMILES

COC1=C(Cl)C=C(C2=CN3C=CC(N4C[C@@H](NCC5=CC=NC=C5)CC4)=CC3=N2)C(OC)=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (215.54 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 2.1554 mL 10.7768 mL 21.5536 mL
5 mM 0.4311 mL 2.1554 mL 4.3107 mL
10 mM 0.2155 mL 1.0777 mL 2.1554 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 and light). 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
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Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

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体積 （終了）

V2

体内:

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 4 mg/mL (8.62 mM); Clear solution

    This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 4 mg/mL (8.62 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 4 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 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.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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 and light)

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.
純度とドキュメンテーション
参考文献

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 and light). 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 2.1554 mL 10.7768 mL 21.5536 mL 53.8840 mL
5 mM 0.4311 mL 2.1554 mL 4.3107 mL 10.7768 mL
10 mM 0.2155 mL 1.0777 mL 2.1554 mL 5.3884 mL
15 mM 0.1437 mL 0.7185 mL 1.4369 mL 3.5923 mL
20 mM 0.1078 mL 0.5388 mL 1.0777 mL 2.6942 mL
25 mM 0.0862 mL 0.4311 mL 0.8621 mL 2.1554 mL
30 mM 0.0718 mL 0.3592 mL 0.7185 mL 1.7961 mL
40 mM 0.0539 mL 0.2694 mL 0.5388 mL 1.3471 mL
50 mM 0.0431 mL 0.2155 mL 0.4311 mL 1.0777 mL
60 mM 0.0359 mL 0.1796 mL 0.3592 mL 0.8981 mL
80 mM 0.0269 mL 0.1347 mL 0.2694 mL 0.6735 mL
100 mM 0.0216 mL 0.1078 mL 0.2155 mL 0.5388 mL
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OTS186935 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
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:

OTS1869352093400-18-9OTS 186935OTS-186935Histone MethyltransferaseH2AXmethyltransferasetoxicityanti-cancerphosphorylationMDA-MB-231breastcancercellsA549lungInhibitorinhibitorinhibit

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製品名:
OTS186935
製品番号:
HY-122181
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