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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.
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 3
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
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.
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.
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.
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)
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.
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.
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.
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.
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
ConcentrationSolventMass
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
10 mM
0.0884 mL
0.4420 mL
0.8840 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 (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.
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.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO 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:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
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.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
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.
*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.
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.
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