Progerinin
Progerinin (SLC-D011) is an orally active progerin-lamin A binding inhibitor. Progerinin selectively binds to the C-terminal region of progerin, disrupting its interaction with lamin A and promoting progerin degradation while sparing wild-type lamin A, B, and C. Progerinin ameliorates nuclear deformation, increases H3K9me3 levels, and reduces progerin expression in HGPS patient-derived fibroblasts. Progerinin extends lifespan in LmnaG609G/G609G mice and LmnaG609G/+ mice, improves body weight, hair morphology, cardiac function, and histological phenotypes. Progerinin can be used for the study of Hutchinson-Gilford progeria syndrome (HGPS).
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- Pureza: 99.74%
- No. CAS: 2249696-72-6
- Fòrmula: C23H22O4
- Peso molecular:362.42
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
Progerinin (100 nM, 3 d) reduces progerin expression, induces H3K9me3 and cyclin B1 expression, and increases Ki67-positive cells in HGPS-derived fibroblasts[1].
Progerinin (2 μM, 7 d) decreases progerin and p16/INK4A levels, restores H3K9me3 expression, and has no significant effect on normal fibroblasts in HGPS-derived fibroblasts[1].
Progerinin (5 μM, 7 d) inhibits progerin-lamin A interaction, ameliorates nuclear deformation, blocks cellular senescence (reduces SA-β-gal staining), and promotes cell proliferation in HGPS cells[1].
Progerinin (500 nM, 3 d) commonly reduces progerin level, induces H3K9me3 and cyclin B1 expression in different HGPS cells (AG11513, AG03199, AG11498, AG03198)[1].
Progerinin (100 nM, 24 h) reduces exogenous GFP-progerin expression in HEK293 cells transiently transfected with GFP-progerin vector[1].
Progerinin (5 μM, 30 min) blocks the interaction between lamin A (GST-LA) and GFP-progerin in HEK293 cells during GST-pull-down assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Progerinin (50 mg/kg, p.o., daily in Monoolein (HY-128754)-based solution, 8 weeks) improves gross morphology, increases body weight and extends lifespan in LmnaG609G/G609G mice[1]. Progerinin (10 mg/mL, p.o., daily in Monoolein-based solution) extends lifespan of LmnaG609G/+ mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LmnaG609G/G609G mice
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Dosage:20 mg/kg
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Administration:i.p., twice weekly starting from 5 or 32 weeks old
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Result:Increased body weight, extends lifespan.
Ameliorated gross morphology.
Improved gross morphology (hair status and body size).
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Animal Model:LmnaG609G/G609G mice
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Dosage:50 mg/kg
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Administration:p.o., daily in monoolein-based solution, 8 weeks
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Result:Improved gross morphology.
Increased body weight and extended lifespan.
Reduced progerin level.
Increased H3K9me3 expression in lung/liver/kidney.
Improved grip strength and heart rate.
Alleviated kyphosis and dental abnormalities.
Reduced tissue fibrosis.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2249696-72-6
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Appearance Solid
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Peso molecular 362.42
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Fòrmula C23H22O4
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Color White to off-white
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SMILES
CC1(OC2=CC(OC(C=C3)=O)=C3C=C2C[C@@H]1OC/C=C/C4=CC=CC=C4)C
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Synonyms
SLC-D011
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (275.92 mM; ultrasonic and warming and heat to 60°C; 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.
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: ≥ 2.5 mg/mL (6.90 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.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.7592 mL | 13.7961 mL | 27.5923 mL | 68.9807 mL |
| 5 mM | 0.5518 mL | 2.7592 mL | 5.5185 mL | 13.7961 mL | |
| 10 mM | 0.2759 mL | 1.3796 mL | 2.7592 mL | 6.8981 mL | |
| 15 mM | 0.1839 mL | 0.9197 mL | 1.8395 mL | 4.5987 mL | |
| 20 mM | 0.1380 mL | 0.6898 mL | 1.3796 mL | 3.4490 mL | |
| 25 mM | 0.1104 mL | 0.5518 mL | 1.1037 mL | 2.7592 mL | |
| 30 mM | 0.0920 mL | 0.4599 mL | 0.9197 mL | 2.2994 mL | |
| 40 mM | 0.0690 mL | 0.3449 mL | 0.6898 mL | 1.7245 mL | |
| 50 mM | 0.0552 mL | 0.2759 mL | 0.5518 mL | 1.3796 mL | |
| 60 mM | 0.0460 mL | 0.2299 mL | 0.4599 mL | 1.1497 mL | |
| 80 mM | 0.0345 mL | 0.1725 mL | 0.3449 mL | 0.8623 mL | |
| 100 mM | 0.0276 mL | 0.1380 mL | 0.2759 mL | 0.6898 mL |
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