Snail IN-1
Based on 1 Customer Validation
Snail IN-1 is an orally active Snail inhibitor with a Ka of 0.36 μM.Snail IN-1 disrupts Snail-CBP interaction, accelerates Snail protein degradation, reduces Snail acetylation, increases Snail polyubiquitination, and selectively downregulates Snail protein without altering other EMT transcription factors.Snail IN-1 reduces atherosclerotic plaque burden, modulates inflammation and plaque stability factors, downregulates CCL5, CXCL10, MMP2, and MMP9, and upregulates α-smooth muscle actin.Snail IN-1 exerts anti-inflammatory and plaque-stabilizing properties.Snail IN-1 can be used for the research of atherosclerosis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.27%
- CAS. Nr.: 3083216-69-4
- Formel: C21H23N5O2S
- Molecular Weight:409.50
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Biologische Aktivität
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CXCR2 |
MMP-9 |
MMP-10 |
Recombinant Snail Protein 0.36 μM (Ki) |
Snail IN-1 (compound S29) (0.1-10 μM; 48 h) potently downregulates the protein level of Snail in HUVECs in a concentration-dependent manner in vitro without altering the mRNA level of Snail, suggesting that its regulatory effect occurs at the post-transcriptional stage[1].
Snail IN-1 (5-60 μM; 48 h) shows no significant cytotoxicity against HUVECs even at concentrations up to 60 μM after 48 h of incubation[1].
Snail IN-1 (5 μM; 0-240 min) accelerates the degradation of Snail protein and reduces its stability in HUVECs[1].
Snail IN-1 (2.5-20 μM; 48 h) specifically downregulates the protein level of Snail in HUVECs, without affecting the protein or mRNA levels of other EMT transcription factors (Zeb1, Slug, Twist)[1].
Snail IN-1 (5 μM; 24 h) promotes Snail degradation by disrupting the interaction between Snail and CBP, reducing the acetylation level of Snail, and increasing the polyubiquitination of Snail in human umbilical vein endothelial cells (HUVECs)[1].
Snail IN-1 (2.5 μM; 24 h) significantly downregulates the mRNA levels of pro-atherosclerotic factors (CCL5, CXCL10, MMP-9, MMP-2) in TNF-α-stimulated HUVECs[1].
Snail IN-1 (1.25-5 μM; 24 h) inhibits the expression of CCL5 and CXCL10 proteins in TNF-α-stimulated HUVEC in a concentration-dependent manner[1].
Snail IN-1 (2.5 μM; 24 h) impairs monocyte recruitment by altering the secretory profile of TNF-α-stimulated HUVEC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human umbilical vein endothelial cells (HUVECs)
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Concentration:0.1, 1.25, 2.5, 5, 10 μM
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Incubation Time:48 h
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Result:Reduced Snail protein levels (normalized to β-actin) to 0.27 relative to vehicle control at 10 μM.
Significantly reduced Snail protein levels at 0.1, 1.25, 2.5, and 5 μM.
Showed no significant changes in Snail mRNA levels across all tested concentrations.
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Cell Line:human umbilical vein endothelial cells (HUVECs)
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Concentration:5, 10, 20, 40, 60 μM
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Incubation Time:48 h
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Result:Showed no significant reduction in HUVEC viability, with cell viability remaining above 90% relative to vehicle control across all tested concentrations.
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Cell Line:human umbilical vein endothelial cells (HUVECs)
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Concentration:5 μM; with cycloheximid (CHX)
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Incubation Time:0, 30, 60, 120, 240 min
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Result:Increased the degradation rate of Snail protein compared to vehicle-treated cells.
Lowered relative Snail protein levels at all time points after CHX addition, with a more pronounced decrease over time.
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Cell Line:human umbilical vein endothelial cells (HUVECs)
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Concentration:5 μM; 2.5, 5, 10, 20 μM
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Incubation Time:48 h
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Result:Potently reduced Snail protein levels at 5 μM, but had no appreciable effect on the abundance of Zeb1, Slug, or Twist protein.
Showed no significant changes in mRNA levels of Zeb1, Slug, Twist, or Snail across tested concentrations.
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Cell Line:TNF-α-stimulated human umbilical vein endothelial cells (HUVECs); THP-1 monocytes
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Concentration:2.5 μM
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Incubation Time:24 h
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Result:Resulted in a significant reduction in THP-1 monocyte migration when using conditioned medium from Snail IN-1-treated HUVECs compared to medium from control cells.
Snail IN-1 (2000 mg/kg; i.g.; single dose) is well-tolerated in C57BL/6 mice, causing no acute organ damage or functional disturbances[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ApoE-/- mice (high-fat diet-induced atherosclerotic model; treated for 4 weeks post-modeling)[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:i.g.; daily; 4 weeks
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Result:Reduced aortic plaque area to 11.33% at 25 mg/kg and a lower unspecified value at 50 mg/kg relative to control.
Reduced intraplaque CCL5 area to ~2% (from control ~15%) and CXCL10 area to ~1.5% (from control ~5%) at 50 mg/kg.
Increased collagen area in plaques to ~45% (from control ~40%) and α-SMA area to ~10% (from control ~3%) at 50 mg/kg.
Reduced intraplaque MMP2 area by 64.2% and MMP9 area by 60% relative to control at 50 mg/kg.
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Animal Model:C57BL/6 mice[1]
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Dosage:2000 mg/kg
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Administration:i.g.; single dose
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Result:Showed no adverse effects, changes in body weight, or organ weight abnormalities.
Exhibited normal tissue architecture with no pathological alterations in heart, liver, spleen, lung, kidney, and brain via histopathological analysis.
Demonstrated serum levels of hepatic injury markers (ALT, AST), renal function markers (BUN, Scr), and metabolic indicators (Glu, LAC) comparable to vehicle control with no statistically significant differences.
Chemical Information
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CAS. Nr. 3083216-69-4
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Appearance Solid
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Molecular Weight 409.50
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Formel C21H23N5O2S
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Color Off-white to light yellow
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SMILES
CC1=C(C=CN=C1CSC2=NC3=CC(N4C=CC=N4)=CC=C3N2)OCCCOC
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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
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (244.20 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: ≥ 2.5 mg/mL (6.11 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.11 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (280 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 2.4420 mL | 12.2100 mL | 24.4200 mL | 61.0501 mL |
| 5 mM | 0.4884 mL | 2.4420 mL | 4.8840 mL | 12.2100 mL | |
| 10 mM | 0.2442 mL | 1.2210 mL | 2.4420 mL | 6.1050 mL | |
| 15 mM | 0.1628 mL | 0.8140 mL | 1.6280 mL | 4.0700 mL | |
| 20 mM | 0.1221 mL | 0.6105 mL | 1.2210 mL | 3.0525 mL | |
| 25 mM | 0.0977 mL | 0.4884 mL | 0.9768 mL | 2.4420 mL | |
| 30 mM | 0.0814 mL | 0.4070 mL | 0.8140 mL | 2.0350 mL | |
| 40 mM | 0.0611 mL | 0.3053 mL | 0.6105 mL | 1.5263 mL | |
| 50 mM | 0.0488 mL | 0.2442 mL | 0.4884 mL | 1.2210 mL | |
| 60 mM | 0.0407 mL | 0.2035 mL | 0.4070 mL | 1.0175 mL | |
| 80 mM | 0.0305 mL | 0.1526 mL | 0.3053 mL | 0.7631 mL | |
| 100 mM | 0.0244 mL | 0.1221 mL | 0.2442 mL | 0.6105 mL |
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