JH-XI-10-02
Based on 2 publication(s) in Google Scholar
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.
(Pink: CDK8 ligand (HY-184544); Blue: Cereblon ligand (HY-10984); Black: linker (HY-117104)).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.73%
- CAS. Nr.: 2209085-22-1
- Formel: C53H69N5O9
- Molecular Weight:920.14
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) JH-XI-10-02
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Biologische Aktivität
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CDK8 159 nM (IC50) |
Cereblon |
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.
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Cell Line:Jurkat cells
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Concentration:1 μM
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Incubation Time:6 and 24 hours
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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.
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Cell Line:WT Molt4 and CRBN null Molt4 cells
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Concentration:0.1, 0.5, 1, 2, 5 μM
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Incubation Time:24 hours
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Result:Degradation of CDK8 at 5 μM in WT Molt4 cells. There were no degradation in CRBN null Molt4 cells at any concentration.
Chemical Information
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CAS. Nr. 2209085-22-1
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Appearance Solid
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Molecular Weight 920.14
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Formel C53H69N5O9
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Color Yellow to brown
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062 -
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
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 |
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| 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 |
JH-XI-10-02 Related Classifications
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