2. PROTAC Cell Cycle/DNA Damage
  3. PROTACs CDK
  4. JH-XI-10-02

JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19.

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JH-XI-10-02

JH-XI-10-02 構造式

CAS 番号 : 2209085-22-1

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 2389 在庫あり
Solution
10 mM * 1 mL in DMSO USD 2389 在庫あり
Solid
1 mg $370 在庫あり
5 mg $1180 在庫あり
10 mg $1890 在庫あり
25 mg $3780 在庫あり
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Based on 2 publication(s) in Google Scholar

JH-XI-10-02 関連抗体

Top Publications Citing Use of Products

PROTACs 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
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

CDK 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
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19[1].

IC50 & Target[1]

CDK8

159 nM (IC50)

Cereblon

 

体外実験

JH-XI-10-02, a bivalent small molecule degrader, recruits the E3 ligase CRL4Cereblon to promote the ubiquitination and proteosomal degradation of CDK8[1].
JH-XI-10-02 (1 μM) induces partial degradation of CDK8 in Jurkat cells upon treatment for 6 h. JH-XI-10-02 (1 μM) induces significant degradation of CDK8 after treatment for 24 h[1].
JH-XI-10-02 induces degradation of CDK8 at 5 μM in WT Molt4 cells, no degradation in CRBN null Molt4 cells at any concentration (0.1-5 μM) in WT Molt4 cells and Molt4 cells where CRBN had been subject to CRISPER/CAS9-mediated deletion for 24 h[1].

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

JH-XI-10-02 関連抗体

Western Blot Analysis[1]

Cell Line: Jurkat cells
Concentration: 1 μM
Incubation Time: 6 and 24 hours
Result: Partial degradation of CDK8 upon treatment for 6 h at a concentration of 1 μM.
Significant degradation of CDK8 after treatment for 24 h at a concentration of 1 μM.

Western Blot Analysis[1]

Cell Line: WT Molt4 and CRBN null Molt4 cells
Concentration: 0.1, 0.5, 1, 2, 5 μM
Incubation Time: 24 hours
Result: Degradation of CDK8 at 5 μM in WT Molt4 cells. There were no degradation in CRBN null Molt4 cells at any concentration.
分子量

920.14

分子式

C53H69N5O9
CAS 番号
Appearance

Solid

Color

Yellow to brown

SMILES

O=C(N([C@H]1CC[C@]2(C)[C@@]3([H])CC[C@]4(C)[C@@H](C5=CC6=C(C=C5)C=CN=C6)CC[C@@]4([H])[C@]3([H])CC[C@@]2([H])C1)C)CCOCCOCCOCCOCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=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 : 100 mg/mL (108.68 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 1.0868 mL 5.4340 mL 10.8679 mL
5 mM 0.2174 mL 1.0868 mL 2.1736 mL
10 mM 0.1087 mL 0.5434 mL 1.0868 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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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

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体積 （開始）

V1

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C2

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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: ≥ 5.75 mg/mL (6.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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).
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

純度: 99.73%

COA (245 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
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 1.0868 mL 5.4340 mL 10.8679 mL 27.1698 mL
5 mM 0.2174 mL 1.0868 mL 2.1736 mL 5.4340 mL
10 mM 0.1087 mL 0.5434 mL 1.0868 mL 2.7170 mL
15 mM 0.0725 mL 0.3623 mL 0.7245 mL 1.8113 mL
20 mM 0.0543 mL 0.2717 mL 0.5434 mL 1.3585 mL
25 mM 0.0435 mL 0.2174 mL 0.4347 mL 1.0868 mL
30 mM 0.0362 mL 0.1811 mL 0.3623 mL 0.9057 mL
40 mM 0.0272 mL 0.1358 mL 0.2717 mL 0.6792 mL
50 mM 0.0217 mL 0.1087 mL 0.2174 mL 0.5434 mL
60 mM 0.0181 mL 0.0906 mL 0.1811 mL 0.4528 mL
80 mM 0.0136 mL 0.0679 mL 0.1358 mL 0.3396 mL
100 mM 0.0109 mL 0.0543 mL 0.1087 mL 0.2717 mL
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JH-XI-10-02 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:

JH-XI-10-022209085-22-1PROTACsCDKCyclin dependent kinaseproteasomaldegradationCDK19CereblonE3 ligaseInhibitorinhibitorinhibit

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製品名:
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製品番号:
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