2. Epigenetics
  3. Histone Demethylase
  4. KDM2A/7A-IN-1

KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases.

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KDM2A/7A-IN-1

KDM2A/7A-IN-1 構造式

CAS 番号 : 2169272-46-0

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 869 在庫あり
Solution
10 mM * 1 mL in DMSO USD 869 在庫あり
Solid
1 mg $320 在庫あり
5 mg $780 在庫あり
10 mg $1200 在庫あり
25 mg $2400 在庫あり
50 mg $3340 在庫あり
100 mg $4400 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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KDM2A/7A-IN-1 関連抗体

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Histone Demethylase 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
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

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製品説明

KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases[1].

IC50 & Target

KDM2

 

体外実験

KDM2A/7A-IN-1 ((S,S)-6) is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive to methyl transferases, and histone acetyl transferases[1].
KDM2A/7A-IN-1 (0.4, 3.1, 6.2 μM) augments cellular H3K36me2 levels in HeLa cells ectopically expressing catalytically active KDM2A[1].

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

KDM2A/7A-IN-1 関連抗体
分子量

506.68

分子式

C33H38N4O
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(N([C@@H](C1=CN=CC(CCCCCCCN2CCCC2)=C1)[C@@]3(C4=CC=CC=C4)C#N)C5=C3C=CC=C5)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 200 mg/mL (394.73 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 1.9736 mL 9.8682 mL 19.7363 mL
5 mM 0.3947 mL 1.9736 mL 3.9473 mL
10 mM 0.1974 mL 0.9868 mL 1.9736 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)

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

×
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: ≥ 5 mg/mL (9.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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).
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. 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 1.9736 mL 9.8682 mL 19.7363 mL 49.3408 mL
5 mM 0.3947 mL 1.9736 mL 3.9473 mL 9.8682 mL
10 mM 0.1974 mL 0.9868 mL 1.9736 mL 4.9341 mL
15 mM 0.1316 mL 0.6579 mL 1.3158 mL 3.2894 mL
20 mM 0.0987 mL 0.4934 mL 0.9868 mL 2.4670 mL
25 mM 0.0789 mL 0.3947 mL 0.7895 mL 1.9736 mL
30 mM 0.0658 mL 0.3289 mL 0.6579 mL 1.6447 mL
40 mM 0.0493 mL 0.2467 mL 0.4934 mL 1.2335 mL
50 mM 0.0395 mL 0.1974 mL 0.3947 mL 0.9868 mL
60 mM 0.0329 mL 0.1645 mL 0.3289 mL 0.8223 mL
80 mM 0.0247 mL 0.1234 mL 0.2467 mL 0.6168 mL
100 mM 0.0197 mL 0.0987 mL 0.1974 mL 0.4934 mL
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KDM2A/7A-IN-1 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:

KDM2A/7A-IN-12169272-46-0Histone DemethylaseInhibitorinhibitorinhibit

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製品名:
KDM2A/7A-IN-1
製品番号:
HY-108706
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