2. Epigenetics Immunology/Inflammation GPCR/G Protein Metabolic Enzyme/Protease
  3. Epigenetic Reader Domain CXCR MMP
  4. Snail IN-1

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.

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Snail IN-1

Snail IN-1 Chemical Structure

CAS No. : 3083216-69-4

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Snail IN-1 Related Antibodies

Top Publications Citing Use of Products

View All CXCR Isoform Specific Products:

View All Isoforms
CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

CXCR2

 

MMP-9

 

MMP-10

 

Recombinant Snail Protein

0.36 μM (Ki)

In Vitro

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.

Snail IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: human umbilical vein endothelial cells (HUVECs)
Concentration: 0.1, 1.25, 2.5, 5, 10 μM
Incubation Time: 48 h
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.

Cell Cytotoxicity Assay[1]

Cell Line: human umbilical vein endothelial cells (HUVECs)
Concentration: 5, 10, 20, 40, 60 μM
Incubation Time: 48 h
Result: Showed no significant reduction in HUVEC viability, with cell viability remaining above 90% relative to vehicle control across all tested concentrations.

Western Blot Analysis[1]

Cell Line: human umbilical vein endothelial cells (HUVECs)
Concentration: 5 μM; with cycloheximid (CHX)
Incubation Time: 0, 30, 60, 120, 240 min
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.

Western Blot Analysis[1]

Cell Line: human umbilical vein endothelial cells (HUVECs)
Concentration: 5 μM; 2.5, 5, 10, 20 μM
Incubation Time: 48 h
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.

Cell Migration Assay[1]

Cell Line: TNF-α-stimulated human umbilical vein endothelial cells (HUVECs); THP-1 monocytes
Concentration: 2.5 μM
Incubation Time: 24 h
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.
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-∞ Bioavailability Tmax
Rat[1] 3 mg/kg i.v. 2.27 ± 1.99 h 16593 ± 3364 ng/mL 5085 ± 1304 ng·h/mL 82.30 % /
Rat[1] 30 mg/kg p.o. 5.05 ± 2.99 h 26104 ± 13526 ng/mL 42193 ± 13110 ng·h/mL 82.30 % 0.50 h
In Vivo

Snail IN-1 (25-50 mg/kg; i.g.; daily; 4 weeks) exerts dose-dependent antiatherosclerotic effects in high-fat diet-fed ApoE-/- mice, reducing plaque burden by decreasing inflammatory chemokines (CCL5, CXCL10) and matrix-degrading enzymes (MMP2, MMP9), while increasing plaque-stabilizing factors (collagen, α-SMA)[1].
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.

Animal Model: ApoE-/- mice (high-fat diet-induced atherosclerotic model; treated for 4 weeks post-modeling)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: i.g.; daily; 4 weeks
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.
Animal Model: C57BL/6 mice[1]
Dosage: 2000 mg/kg
Administration: i.g.; single dose
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.
Molecular Weight

409.50

Formula

C21H23N5O2S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=C(C=CN=C1CSC2=NC3=CC(N4C=CC=N4)=CC=C3N2)OCCCOC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4420 mL 12.2100 mL 24.4200 mL
5 mM 0.4884 mL 2.4420 mL 4.8840 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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Volume (final)

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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 2.4420 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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Snail IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Snail IN-13083216-69-4Snail IN1Snail IN 1Epigenetic Reader DomainCXCRMMPCXC chemokine receptorsC-X-C motif chemokine receptorsMatrix metalloproteinasesCBPα-smooth muscle actinMMP9MMP2atherosclerosisSnailCXCL10HUVECsEMT transcription factorsCCL5Inhibitorinhibitorinhibit

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