2. Anti-infection Metabolic Enzyme/Protease Neuronal Signaling
  3. HIV Protease Monoamine Oxidase
  4. Escin IA

Escin IA is an oral LOXL2 inhibitor and EMT inhibitor, with selectivity for LOXL2-expressing cells. Escin IA suppresses invasion, migration, and metastasis of breast cancer cells, and acts as the primary anti-TNBC metastasis constituent of Aesculus chinensis Bunge fruit saponin fraction. Escin IA can be used for the research of triple-negative breast cancer, acute inflammation, and ethanol-induced gastric mucosal lesions.

For research use only. We do not sell to patients.

Escin IA

Escin IA Chemical Structure

CAS No. : 123748-68-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Escin IA Related Antibodies

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1 Publications Citing Use of MCE Escin IA

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Description

Escin IA is an oral LOXL2 inhibitor and EMT inhibitor, with selectivity for LOXL2-expressing cells. Escin IA suppresses invasion, migration, and metastasis of breast cancer cells, and acts as the primary anti-TNBC metastasis constituent of Aesculus chinensis Bunge fruit saponin fraction. Escin IA can be used for the research of triple-negative breast cancer, acute inflammation, and ethanol-induced gastric mucosal lesions[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
Vero C1008 CC50
25 μM
Compound: 71
Cytotoxicity against African green monkey Vero E6 cells incubated for 2 days by the MTS assay
Cytotoxicity against African green monkey Vero E6 cells incubated for 2 days by the MTS assay
[PMID: 32845145]
In Vitro

Escin Ia (2.5-10 μM; 24 h) inhibits the invasion of MDA-MB-231 cells in a concentration-dependent manner, with 10 μM causing the highest inhibition (76.23%)[1].
Escin Ia (2.5-10 μM; 24 h) modulates mRNA expression of LOXL2, E-cadherin, and MMP9 in MDA-MB-231 cells, with LOXL2 down-regulation and E-cadherin up-regulation being prominent effects[1].
Escin Ia (2.5-10 μM; 6-24 h, unspecified intervals) suppresses the epithelial-mesenchymal transition (EMT) process in MDA-MB-231 cells by modulating EMT markers and transcription factors[1].
Escin Ia (2.5-10 μM; 6-24 h, unspecified intervals) reverses the EMT process in TNF−α/TGF−β-stimulated MCF-7 cells by normalizing EMT marker expressions[1].
Escin Ia (2.5-10 μM; 6-24 h, unspecified intervals) down-regulates LOXL2 expression in MDA-MB-231 cells and abrogates induced LOXL2 expression in TNF-α/TGF-β-stimulated or LOXL2-transfected MCF-7 cells[1].
Escin Ia (2.5-10 μM; unspecified intervals) inhibits the EMT process in LOXL2-transfected MCF-7 cells by down-regulating LOXL2 and normalizing EMT markers[1].
Escin Ia (2.5-10 μM; unspecified intervals) inhibits the EMT process in hypoxia-stimulated MCF-7 cells by down-regulating LOXL2 (without affecting HIF-1α) and normalizing EMT markers[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Escin IA Related Antibodies

Cell Invasion Assay[1]

Cell Line: MDA-MB-231
Concentration: 5 μM; 2.5-10 μM
Incubation Time: 24 h
Result: Inhibited MDA-MB-231 cell invasion by 68.92% at 5 μM (stronger than other escin analogs); inhibited invasion by 39.46% at 2.5 μM, 64.22% at 5 μM, and 76.23% at 10 μM.

Real Time qPCR[1]

Cell Line: MDA-MB-231
Concentration: 2.5-10 μM
Incubation Time: 24 h
Result: Down-regulated LOXL2 mRNA expression and up-regulated E-cadherin mRNA expression; moderately down-regulated MMP9 mRNA expression at 10 μM; exerted slight effects on BRMS1, Keratin19, Orai1, Stim1, TGF-β, and VEGF mRNAs.
Parmacokinetics
Species Dose Route Cmax T1/2 AUC0-t AUC0-∞ CL Vd MRT
Rat[3] 0.5 mg/kg i.v. 2280 ng/mL 7.5 h 10,036 ng·h/mL 10,145 ng·h/mL 4.82 mL/min/kg 2.86 L/kg 5.46 h
Rat[3] 1.0 mg/kg i.v. 4362 ng/mL 9.6 h 12989 ng·h/mL 13185 ng·h/mL 6.05 mL/min/kg 5.02 L/kg 5.39 h
Rat[3] 2.0 mg/kg i.v. 11220 ng/mL 12.2 h 29156 ng·h/mL 29941 ng·h/mL 5.81 mL/min/kg 6.16 L/kg 6.29 h
In Vivo

Escin Ia (2-4 mg/kg; i.p.; three times per week; five weeks) suppresses TNBC metastasis and EMT in MDA-MB-231 xenograft mice by down-regulating LOXL2, with 4 mg/kg showing greater efficacy than 2 mg/kg[1].
Escin Ia (50-200 mg/kg; p.o.) dose-dependently inhibits acetic acid-induced vascular permeability in Mus musculus, with 43.6% inhibition at 200 mg/kg[2].
Escin Ia (25-200 mg/kg; p.o.) inhibits compound 48/80-induced scratching in mice, with significant 42.4% inhibition at 200 mg/kg[2].
Escin Ia (200 mg/kg; p.o.) significantly inhibits the early phase (1 hour) of carrageenin-induced hind paw edema in rats[2].
Escin Ia (25-200 mg/kg; p.o.) dose-dependently inhibits histamine-induced vascular permeability in rats (significant at 50-200 mg/kg) but does not inhibit serotonin-induced vascular permeability[2].
Escin IA (10-50 mg/kg; p.o.; single dose 1 hour before ethanol administration) potently protects against ethanol-induced gastric mucosal lesions in rats via mechanisms involving capsaicin-sensitive afferent neurons, endogenous nitric oxide, and prostaglandins, with no gastric antisecretory activity at effective doses[4].
Escin IA (10 mg/kg; p.o.; single dose 1 hour before ethanol administration) relies on capsaicin-sensitive afferent neurons for its gastroprotective effect in rats[4].
Escin IA (10 mg/kg; p.o.; single dose 1 hour before ethanol administration) relies on endogenous prostaglandins for its gastroprotective effect in rats[4].
Escin IA (10 mg/kg; p.o.; single dose 1 hour before ethanol administration) relies on endogenous nitric oxide for its gastroprotective effect in rats[4].
Escin IA (10 mg/kg; p.o.; single dose 1 hour before ethanol administration) does not rely on endogenous sulfhydryls for its gastroprotective effect in rats[4].
Escin IA (10-20 mg/kg; p.o.; single dose 1 hour before ethanol administration) relies on the sympathetic nervous system for its gastroprotective effect in rats[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: athymic nude mice (female, 4-6 week-old)[1]
Dosage: 2 mg/kg; 4 mg/kg
Administration: i.p.; three times per week; five weeks
Result: Down-regulated LOXL2, vimentin, α-SMA, Snail, Slug, Zeb1, Zeb2, and Twist, and up-regulated E-cadherin at protein and mRNA levels in breast tumors (4 mg/kg); showed little effect on HIF-1α expression in breast tumors (2 mg/kg, 4 mg/kg)
Animal Model: ddY mice (male, 27-30 g, acetic acid-induced vascular permeability model)[2]
Dosage: 50, 100, 200 mg/kg
Administration: p.o.
Result: Inhibited acetic acid-induced vascular permeability with 12.1% inhibition at 50 mg/kg, 30.6% inhibition at 100 mg/kg, and 43.6% inhibition at 200 mg/kg.
Animal Model: ddY mice (male, 26-29 g, compound 48/80-induced scratching model)[2]
Dosage: 25, 50, 100, 200 mg/kg
Administration: p.o.
Result: Inhibited compound 48/80-induced scratching with 16.8% inhibition at 25 mg/kg, 32.4% inhibition at 50 mg/kg, 31.5% inhibition at 100 mg/kg, and 42.4% inhibition at 200 mg/kg (significant at 200 mg/kg).
Animal Model: Wistar rats (male, 140-160 g, carrageenin-induced hind paw edema model)[2]
Dosage: 200 mg/kg
Administration: p.o.
Result: Significantly inhibited carrageenin-induced hind paw swelling at 1 hour but showed no effect at 3-5 hours.
Animal Model: Wistar rats (male, 140-150 g, histamine/serotonin-induced vascular permeability model)[2]
Dosage: 25, 50, 100, 200 mg/kg
Administration: p.o.
Result: Inhibited histamine-induced vascular permeability with significant effects at 50 mg/kg (28.4 μg/site dye leakage), 100 mg/kg (28.5 μg/site), and 200 mg/kg (19.4 μg/site); did not significantly inhibit serotonin-induced vascular permeability at any dose.
Animal Model: Sprague-Dawley (male, 250 g, fasted 24-26 hours prior to experiments; ethanol-induced gastric mucosal lesions)[4]
Dosage: 10, 20, 50 mg/kg
Administration: p.o.; single dose 1 hour before ethanol administration
Result: Dose-dependently reduced ethanol-induced gastric lesion scores; showed potent protective effect at 10-50 mg/kg. Did not decrease gastric secretion (volume, acid output, pepsin output) in pylorus-ligated rats at 10 and 20 mg/kg. Had gastroprotective effect attenuated by pretreatment with capsaicin, indomethacin, or L-NAME at 10 mg/kg. Had gastroprotective effect not attenuated by pretreatment with N-ethylmaleimide at 10 mg/kg. Showed marked attenuation of gastroprotective effect in streptozotocin-induced diabetic rats at 10 and 20 mg/kg.
Animal Model: Sprague-Dawley (male, 180-200 g for capsaicin pretreatment; 250 g for other pretreatments, fasted 24-26 hours prior to experiments; capsaicin-pretreated, ethanol-induced gastric mucosal lesions)[4]
Dosage: 10 mg/kg
Administration: p.o.; single dose 1 hour before ethanol administration
Result: Showed gastroprotective effect against ethanol-induced lesions markedly attenuated by capsaicin pretreatment.
Animal Model: Sprague-Dawley (male, 250 g, fasted 24-26 hours prior to experiments; indomethacin-pretreated, ethanol-induced gastric mucosal lesions)[4]
Dosage: 10 mg/kg
Administration: p.o.; single dose 1 hour before ethanol administration
Result: Showed gastroprotective effect against ethanol-induced lesions partly reduced by indomethacin pretreatment.
Animal Model: Sprague-Dawley (male, 250 g, fasted 24-26 hours prior to experiments; L-NAME-pretreated, ethanol-induced gastric mucosal lesions)[4]
Dosage: 10 mg/kg
Administration: p.o.; single dose 1 hour before ethanol administration
Result: Showed gastroprotective effect against ethanol-induced lesions partly reduced by L-NAME pretreatment.
Animal Model: Sprague-Dawley (male, 250 g, fasted 24-26 hours prior to experiments; N-ethylmaleimide-pretreated, ethanol-induced gastric mucosal lesions)[4]
Dosage: 10 mg/kg
Administration: p.o.; single dose 1 hour before ethanol administration
Result: Showed gastroprotective effect against ethanol-induced lesions not attenuated by N-ethylmaleimide pretreatment.
Animal Model: Sprague-Dawley (male, 250 g, fasted 24-26 hours prior to experiments; streptozotocin-induced diabetic, ethanol-induced gastric mucosal lesions)[4]
Dosage: 10, 20 mg/kg
Administration: p.o.; single dose 1 hour before ethanol administration
Result: Showed marked attenuation of gastroprotective effect against ethanol-induced lesions in streptozotocin-induced diabetic rats at 10 and 20 mg/kg.
Molecular Weight

1131.26

Formula

C55H86O24
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC[C@]1([C@H]2OC(C)=O)[C@](CC(C)(C)[C@H]2OC(/C(C)=C/C)=O)([H])C3=CC[C@@]4([H])[C@@](C)(CC[C@]5([H])[C@@]4(CC[C@H](O[C@@](O[C@H](C(O)=O)[C@@H](O[C@]([C@@H]([C@@H](O)[C@@H]6O)O)([H])O[C@@H]6CO)[C@@H]7O)([H])[C@@H]7O[C@]([C@@H]([C@@H](O)[C@@H]8O)O)([H])O[C@@H]8CO)[C@]5(C)CO)C)[C@]3(C)C[C@H]1O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (88.40 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 0.8840 mL 4.4199 mL 8.8397 mL
5 mM 0.1768 mL 0.8840 mL 1.7679 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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 (2.21 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.
In Vivo Dissolution Calculator
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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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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

Purity: 99.59%

SDS (393 KB)

COA (258 KB) LCMS (90 KB)

Handling Instructions (2659 KB)
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 (protect from light). 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 0.8840 mL 4.4199 mL 8.8397 mL 22.0993 mL
5 mM 0.1768 mL 0.8840 mL 1.7679 mL 4.4199 mL
10 mM 0.0884 mL 0.4420 mL 0.8840 mL 2.2099 mL
15 mM 0.0589 mL 0.2947 mL 0.5893 mL 1.4733 mL
20 mM 0.0442 mL 0.2210 mL 0.4420 mL 1.1050 mL
25 mM 0.0354 mL 0.1768 mL 0.3536 mL 0.8840 mL
30 mM 0.0295 mL 0.1473 mL 0.2947 mL 0.7366 mL
40 mM 0.0221 mL 0.1105 mL 0.2210 mL 0.5525 mL
50 mM 0.0177 mL 0.0884 mL 0.1768 mL 0.4420 mL
60 mM 0.0147 mL 0.0737 mL 0.1473 mL 0.3683 mL
80 mM 0.0110 mL 0.0552 mL 0.1105 mL 0.2762 mL
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Escin IA 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:

Escin IA123748-68-5HIV ProteaseMonoamine OxidaseMAOepithelial-mesenchymal transitiontriple-negative breast cancerE-cadherinethanol-induced gastric mucosal lesionsEMTMDA-MB-231 cellsbreast cancer cellsMCF-7 cellsLOXL2Aesculus chinensis BungeInhibitorinhibitorinhibit

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