Senexin A
Based on 9 publication(s) in Google Scholar
Senexin A is an inhibitor of CDK8/19 (IC50: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.58%
- CAS. Nr.: 1366002-50-7
- Formel: C17H14N4
- Molecular Weight:274.32
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Kinase Inhibitor Library
HY-L009
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NF-κB Signaling Compound Library
HY-L014
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HY-L025
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Publications Citing Use of MedChemExpress (MCE) Senexin A
More- Nucleic Acids Res. 2021 Feb 22;49(3):1470-1484. [Abstract]
- Cell Death Dis. 2020 Sep 15;11(9):754. [Abstract]
- Int J Biol Sci. 2025 Jan 1;21(2):685-707. [Abstract]
- Biochem Pharmacol. 2025 Apr 23:116959. [Abstract]
- Mol Med Rep. 2020 Dec;22(6):4868-4876. [Abstract]
- Viruses. 2020 Jun 17;12(6):654. [Abstract]
- FEBS Lett. 2021 Jul;595(14):1933-1948. [Abstract]
- J Cell Biochem. 2019 Aug;120(8):14095-14106. [Abstract]
- bioRxiv. 2025 Dec 9.
Biologische Aktivität
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CDK19 0.31 μM (Kd) |
CDK8 0.83 μM (Kd) |
CDK8 280 nM (IC50) |
Senexin A inhibits CDK8 and CDK19 ATP site binding with Kd50 of 0.83 μM and 0.31 μM, respectively[1].
Senexin A inhibits β-catenin-dependent transcription in HCT116 colon cancer cells[1].
In HT1080 cells, Senexin A strongly inhibits the induction of the transcription factor EGR1 upon serum starvation[1].
Senexin A also reduces the expression of many secreted tumor-promoting factors in doxorubicin-treated wild-type HCT116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1366002-50-7
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Appearance Solid
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Molecular Weight 274.32
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Formel C17H14N4
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Color White to off-white
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SMILES
N#CC1=CC=C2C(C(NCCC3=CC=CC=C3)=NC=N2)=C1
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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 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Nucleic Acids Res
Loss of Mediator complex subunit 13 (MED13) promotes resistance to alkylation through cyclin D1 upregulation. [Abstract]2021 Feb 22;49(3):1470-1484. PMID: 33444446 -
Cell Death Dis
2020 Sep 15;11(9):754. PMID: 32934219 -
Int J Biol Sci
The Cyclin-Dependent Kinase 8 Inhibitor E966-0530-45418 Attenuates Pulmonary Fibrosis In Vitro and In Vivo. [Abstract]2025 Jan 1;21(2):685-707. PMID: 39781457 -
Biochem Pharmacol
Identification of pyrazole scaffold inhibitors targeting cyclin-dependent kinase 8 for potential use in pulmonary fibrosis. [Abstract]2025 Apr 23:116959. PMID: 40280247 -
Mol Med Rep
Capsaicin suppresses breast cancer cell viability by regulating the CDK8/PI3K/Akt/Wnt/β‑catenin signaling pathway. [Abstract]2020 Dec;22(6):4868-4876. PMID: 33173974 -
Viruses
Cyclin-Dependent Kinases 8 and 19 Regulate Host Cell Metabolism during Dengue Virus Serotype 2 Infection. [Abstract]2020 Jun 17;12(6):654. PMID: 32560467 -
FEBS Lett
MED12 interacts with the heat-shock transcription factor HSF1 and recruits CDK8 to promote the heat-shock response in mammalian cells. [Abstract]2021 Jul;595(14):1933-1948. PMID: 34056708 -
J Cell Biochem
The microRNA-141-3p/ CDK8 pathway regulates the chemosensitivity of breast cancer cells to trastuzumab. [Abstract]2019 Aug;120(8):14095-14106. PMID: 31087707 -
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (364.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.5 mg/mL (9.11 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 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.
Protokoll
Mice: Senexin A toxicity study is conducted by Taconic in C57BL/6 mice, using five mice per group treated with 20 mg/kg Senexin A or carrier (80% propylene glycol), with five daily i.p. injections. Mice are weighed on days 3 and 6, and killed on day 6. Organ weights are determined for brain, kidney, thymus, spleen, lung, and liver. Terminal blood samples are analyzed to determine the numbers of total white blood cells, neutrophils, lymphocytes, monocytes, eosinophils, and basophils[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (277 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
[1]. Porter DC, et al. Cyclin-dependent kinase 8 mediates chemotherapy-induced tumor-promoting paracrine activities. Proc Natl Acad Sci U S A. 2012 Aug 21;109(34):13799-804. [Content Brief]
[2]. Ho TY, et al. The study of a novel CDK8 inhibitor E966-0530-45418 that inhibits prostate cancer metastasis in vitro and in vivo. Biomed Pharmacother. 2023 Jun;162:114667. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6454 mL | 18.2269 mL | 36.4538 mL | 91.1344 mL |
| 5 mM | 0.7291 mL | 3.6454 mL | 7.2908 mL | 18.2269 mL | |
| 10 mM | 0.3645 mL | 1.8227 mL | 3.6454 mL | 9.1134 mL | |
| 15 mM | 0.2430 mL | 1.2151 mL | 2.4303 mL | 6.0756 mL | |
| 20 mM | 0.1823 mL | 0.9113 mL | 1.8227 mL | 4.5567 mL | |
| 25 mM | 0.1458 mL | 0.7291 mL | 1.4582 mL | 3.6454 mL | |
| 30 mM | 0.1215 mL | 0.6076 mL | 1.2151 mL | 3.0378 mL | |
| 40 mM | 0.0911 mL | 0.4557 mL | 0.9113 mL | 2.2784 mL | |
| 50 mM | 0.0729 mL | 0.3645 mL | 0.7291 mL | 1.8227 mL | |
| 60 mM | 0.0608 mL | 0.3038 mL | 0.6076 mL | 1.5189 mL | |
| 80 mM | 0.0456 mL | 0.2278 mL | 0.4557 mL | 1.1392 mL | |
| 100 mM | 0.0365 mL | 0.1823 mL | 0.3645 mL | 0.9113 mL |
Senexin A Related Classifications
HY-15681 Related Classifications
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