SEC inhibitor KL-1
Based on 1 publication(s) in Google Scholar
SEC inhibitor KL-1 (KL-1) is a peptide-like lead compound that is an effective selective SEC inhibitor. SEC inhibitor KL-1 promotes apoptosis and has anti-tumor activity. SEC inhibitor KL-1 doses dependently inhibits the AFF4-CCNT1 interaction, with a Ki value of 3.48 μM.
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- Pureza: 99.58%
- No. CAS: 900308-84-1
- Fòrmula: C18H16ClNO4
- Peso molecular:345.78
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) SEC inhibitor KL-1
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Actividad biológica
SEC[2]
SEC inhibitor KL-1 (0-100μM, 24-72h) inhibits the growth of DIPG cells and increases apoptosis[1].
SEC inhibitor KL-1 for H3 wild-type astrocytes, the h3g34v mutant glioma cells, and NHA cells with IC50 are 18, 16 and 18μM, respectively[1].
SEC inhibitor KL-1 disrupts SEC, leading to increase occupancy of Pol II near the promoter, which can delay Pol II mutants and slow down Pol II's elongation rate[2].
SEC inhibitor KL-1 (5h) blocks the induction of heat shock-induced genes FOS, HSPD1, HSPE1, and EGR1 in HCT116 cells, impairing the heat shock response[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SF8628, DIPG-007, SU-DIPG4, SU-DIPG36
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Concentration:0-100 μM
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Incubation Time:24, 72 h
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Result:Inhibited the growth of DIPG cells.
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Cell Line:H3K27M mutant DIPG cells
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Concentration:20, 40 μM
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Incubation Time:72 h
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Result:Increased in a dose-dependent manner in Annexin v positive cells, increasing apoptosis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse MDA231-LM2 tumor model[2]
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Dosage:50 mg/kg, once a day, 15 days
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Administration:Intraperitoneal injection (i.p.)
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Result:Reduced tumor volume and significantly extended survival time of recipient mice.
Chemical Information
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No. CAS 900308-84-1
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Appearance Solid
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Peso molecular 345.78
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Fòrmula C18H16ClNO4
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Color Light yellow to yellow
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SMILES
O=C(/C(O)=C/C(C1=CC=CC(OC)=C1)=O)NC2=CC(Cl)=CC=C2C
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Synonyms
KL-1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 41.67 mg/mL (120.51 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, 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: 2.08 mg/mL (6.02 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 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 (20.8 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 5 mg/mL (14.46 mM); Suspended solution; Need ultrasonic
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.
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Hiroaki Katagi, et al. Therapeutic targeting of transcriptional elongation in diffuse intrinsic pontine glioma. Neuro Oncol. 2021 Aug 2;23(8):1348-1359. [Content Brief]
[2]. Liang K, et al. Targeting Processive Transcription Elongation via SEC Disruption for MYC-Induced CancerTherapy. Cell. 2018 Oct 18;175(3):766-779. [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 | 2.8920 mL | 14.4601 mL | 28.9201 mL | 72.3003 mL |
| 5 mM | 0.5784 mL | 2.8920 mL | 5.7840 mL | 14.4601 mL | |
| 10 mM | 0.2892 mL | 1.4460 mL | 2.8920 mL | 7.2300 mL | |
| 15 mM | 0.1928 mL | 0.9640 mL | 1.9280 mL | 4.8200 mL | |
| 20 mM | 0.1446 mL | 0.7230 mL | 1.4460 mL | 3.6150 mL | |
| 25 mM | 0.1157 mL | 0.5784 mL | 1.1568 mL | 2.8920 mL | |
| 30 mM | 0.0964 mL | 0.4820 mL | 0.9640 mL | 2.4100 mL | |
| 40 mM | 0.0723 mL | 0.3615 mL | 0.7230 mL | 1.8075 mL | |
| 50 mM | 0.0578 mL | 0.2892 mL | 0.5784 mL | 1.4460 mL | |
| 60 mM | 0.0482 mL | 0.2410 mL | 0.4820 mL | 1.2050 mL | |
| 80 mM | 0.0362 mL | 0.1808 mL | 0.3615 mL | 0.9038 mL | |
| 100 mM | 0.0289 mL | 0.1446 mL | 0.2892 mL | 0.7230 mL |
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