Cat. No.: HY-N1939

Icariside I

(Synonyms: Icarisid I)

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

Icariside I (GH01) is an orally active metabolite of icalin. Icariside I improves estrogen deficiency-induced osteoporosis by simultaneously regulating osteoblast and osteoclast differentiation. Icariside I promotes ATP (HY-B2176) or Nigericin (HY-127019)-induced mtROS production and NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Icariside I does not alter the activation of NLRC4 and AIM2 inflammasomes. Icariside I inhibits breast cancer proliferation, apoptosis, invasion, and metastasis by targeting the IL-6/STAT3 pathway. Icariside I is a kynurenine-AhR pathway inhibitor that alleviates cancer by blocking tumor immune escape.

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

Purity: 98.76%
CAS No.: 56725-99-6
Formula: C₂₇H₃₀O₁₁
Molecular Weight:530.52

Storage:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Icariside I Chemical Structure

CAS No.: 56725-99-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

NLRP3

All NOD-like Receptor (NLR) Isoforms :

All STAT Isoforms :

All CDK Isoforms :

All Bcl-2 Family Isoforms :

All JAK Isoforms :

All Caspase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
NCI/ADR-RES	IC₅₀	60.78 μM Compound: 4	Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay	[PMID: 19523827]

In Vitro

Icariside I (10-40 μM, 1 h) enhances NLRP3 inflammasome activation dependent on mitochondrial ROS production triggered by ATP (HY-B2176) and Nigericin (HY-127019), but not SiO2, Poly(I:C) (HY-107202) and cytosolic LPS (HY-D1056), has no effect on NLRC4 and AIM2 inflammasomes activation in BMDMs^[1].
Icariside I (20 μM, 1 h) promotes ATP or Nigericin-induced ASC oligomerization but has no effect on K₊ efflux in BMDMs^[1].
Icariside I (0-100 μM, 12 h) does not impair the viability of 4T1 cells at a concentration lower than 60 μM^[2].
Icariside I (0-40 μM, 1 h) inhibits IL-6/STAT3 signaling in 4T1-luc cells^[2].
Icariside I (0-40 μM, 1-5 days) suppresses proliferation and migration, reduces the mRNA level of MMP2 and MMP9 in 4T1-luc cells^[2].
Icariside I (0-40 μM, 1 h) can hinder the cell cycle and reduces Cyclin D1, CDK4, bcl-2, and increases bax mRNA expression to regulate proliferation and survival of 4T1-luc cells^[2].
Icariside I (5-20 μM, 24 h) inhibits Kyn-AhR pathway as well as reduction of tumor cell viability in B16F10-cells^[3].
Icariside I (0.1-100 nM) represses osteoclast differentiation and resorption by suppressing MAPK-p38-NFATc1 cascade in primary BMMs^[4].
Icariside I (0.1-1000 nM, 3-14 days) promotes differentiation and formation of osteoblasts, upregulated downstream signal factors such as RUNX2 in primary BMMs^[4].

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

Western Blot Analysis^[1]

Cell Line:

BMDMs
Concentration:

20 μM
Incubation Time:

1 h
Result:

Promoted caspase-1 activation and IL-1β production, was not affected the expression of NLRP3, ASC, pro-IL-1β, and pro-caspase-1 (p45) induced by ATP in LPS-primed.
Had no effect on caspase-1 cleavage, IL-1β secretion and LDH release triggered by SiO2 and poly.
Did not alter caspase-1 cleavage, IL-1β secretion, and LDH release in Pam3CSK4 (HY-P1180)-primed BMDMs transfected with LPS, did not affect the expression of pro-IL-1β, ASC, NLRP3 and pro-caspase-1.
Did not alter the release of caspase-1 cleavage, IL-1β secretion, LDH and ASC oligomerization release in response to Salmonella typhimurium infection and triggered by Poly (dA:dT) (HY-138646) transfection, was not affected the expression of NLRP3, ASC, pro-IL-1β and pro-caspase-1 (p45) in cell lysate.
Promoted ATP-induced ASC oligomerization and the production of caspase-1 and IL-1β induced by Nigericin but not SiO2, poly(I:C) and intracellular LPS in LPS-primed.

Western Blot Analysis^[2]

Cell Line:

4T1-luc cells
Concentration:

0 μM, 10 μM, 20 μM, 40 μM
Incubation Time:

1 h
Result:

Reduced the phosphorylation of STAT3 induced by IL-6, decreased p-STAT3 (Tyr705) exposed to IL-6 (50 ng/mL) after 12 h. Decreased the protein level of vimentin in the presence of IL-6.

Cell Migration Assay ^[2]

Cell Line:

4T1-luc cells
Concentration:

0 μM, 10 μM, 20 μM, 40 μM
Incubation Time:

1 days, 5 days
Result:

Inhibited IL-6-induced wound healing, the development of colonies.

Cell Cycle Analysis^[2]

Cell Line:

4T1-luc cells
Concentration:

0 μM, 10 μM, 20 μM, 40 μM
Incubation Time:

1 h
Result:

Entered a viable G1 arrest state, decreased IL-6-induced the proliferative phase of the cell cycle (S+G2/M), prevented cells from entering the S phase.

Western Blot Analysis^[4]

Cell Line:

BMMs
Concentration:

100 nM
Incubation Time:

0 min, 5 min, 15 min, 30 min
Result:

Reduced the level of phosphorylated p38 (p-p38) protein, had no change in JNK, P-JNK, ERK 1/2, and P-ERK 1/2 protein levels.

In Vivo

Icariside I (25-100 mg/kg, i.p., once) could induce liver injury in an LPS-mediated susceptibility mouse model of idiosyncratic drug-induced liver injury (IDILI)^[1].
Icariside I (25-50 mg/kg, p.o., once a days, 27 days) suppresses tumor growth and lung metastasis in the 4T1 breast cancer model through IL-6/STAT3 pathway^[2].
Icariside I (5-20 mg/kg, p.o., 7 days) downregulates SLC7A8 and PAT4 transporters and AhR, thus inhibiting nuclear PD-1 in CTLs, through activation of JAK1-STAT1 signaling, thus inducing tumor cell apoptosis in tumor-bearing mice^[3].
Icariside I (5-50 mg/kg, i.g., 6 days per week, 4 weeks) ameliorates estrogen deficiency-induced osteoporosis without significant hepatotoxicity in ovariectomy (OVX)-induced osteoporosis mouse model^[4].

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

Animal Model:

LPS-mediated susceptible C57BL/6 mice (Female 6-8-week-old) model of IDILI^[1]
Dosage:

25 mg/kg, 50 mg/kg, 100 mg/kg
Administration:

i.p., once
Result:

Induced the elevation of ALT and AST serum levels, increased the production of IL-1β and TNF-α production.
Did not alter liver tissue structure Icariside I and LPS alone treatment, led to a trend of hepatocyte focal necrosis and inflammatory cell infiltration in the liver tissue used in combination with LPS.
Facilitated the number of macrophages, leucocytes, macrophages and neutrophils used in combination with LPS.

Animal Model:

4T1-luc cells (1 × 10⁵) xenografts BALB/c mice (Female, 6 weeks)^[2]
Dosage:

25 mg/kg, 50 mg/kg
Administration:

p.o., once a days, 27 days
Result:

Reduced tumor weight and tumor volume, reduced phosphorylated STAT3 levels and IL-6.
Decreased the expressions of vimentin, bcl-2, Cyclin D1, and CDK4, increased the expressions of pro-apoptotic proteins bax and cleaved caspase 3.
Reduced lung metastasis and damage, decreased mRNA expression of the invasive proteins MMP9 and vimentin.

Animal Model:

Tumor-bearing mice (C57BL/6 female, 18-22 g)^[3]
Dosage:

5 mg/kg, 20 mg/kg
Administration:

p.o., 7 days
Result:

Reduced tumor volume and tumor weight without body weight changes, inhibited tumor cell proliferation and promoted cell shrinkage, nuclear condensation and necrosis of mouse tumor cells.
Restored the size and weight of immune organs (thymus and spleen), alleviated thymus atrophy and splenomegaly in tumor-bearing mice, and improved the total T cells, CD4+T cells, and CD8+T cells and their ratios in the peripheral blood of the tumor group, enhanced the proportion of TILs and CD8+ T cells and up-regulated the CD8+/CD4+ ratio in tumor tissues.
Upregulated mRNAs levels of CCL4 and CCL8 and CXCL9 and CXCL10, as well as IFN-γ and GZMB and CD69 and Klrk1.
Rescued the levels of intermediate metabolites including Trp, Kyn, kynurenic acid, xanthurenic acid, 3 H-KYN, 3-HAA, quinolinic acid and picolinic acid involved in Trp-Kyn pathway in plasma, reduced the levels of Kyn, kynurenic acid and xanthurenic acid and ratio of Kyn to Trp, downregulated mRNA levels of multiple genes including Ido1, Kat1, Kat3, Kmo, Kynu and Ahr involved in Kyn-AhR pathway.
Down-regulated the mRNA level of SLC7A8, PAT4 transporters of Kyn, kynurenic acid and xanthurenic acid, inhibited AhR, down-regulated the mRNA level of PD-1, p27.

Animal Model:

OVX-induced osteoporosis mouse (C57BL/6 12 week-old female) model^[4]
Dosage:

5 mg/kg, 50 mg/kg
Administration:

i.g., 6 days per week, 4 weeks
Result:

Improved liver injury, ameliorates estrogen deficiency-induced osteoporosis without significant hepatotoxicity.

Chemical Information

CAS No. 56725-99-6
Appearance Solid
Molecular Weight 530.52
Formula C₂₇H₃₀O₁₁
Color Light yellow to yellow
SMILES

O=C1C(O)=C(C2=CC=C(OC)C=C2)OC3=C(C/C=C(C)\C)C(O[C@H]4[C@@H]([C@H]([C@@H]([C@@H](CO)O4)O)O)O)=CC(O)=C13
Synonyms

Icarisid I
Structure Classification
- Flavonoids
- Flavonols
- Phenols
- Monophenols
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Publications (3)

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Journal Impact Factor

Food Chem

Effects of sun drying combined with baking processes on the flavor quality of Chongqing Tuocha raw tea. [Abstract]

2025 Dec 30:497:146992. PMID: 41285060
Food Chem

Flavonoid-mediated metabolic underpinning quality variation in red bud-sport pear mutants. [Abstract]

2025 May 31:489:144992. PMID: 40466530
Phytomedicine

Novel strategies for identification and prevention of idiosyncratic liver injury caused by TCM compatibility: Exemplification by Epimedii Folium and Psoraleae Fructus. [Abstract]

2026 Jan 16:153:157841. PMID: 41655541

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (117.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8849 mL

9.4247 mL

18.8494 mL

5 mM

0.3770 mL

1.8849 mL

3.7699 mL

10 mM

0.1885 mL

0.9425 mL

1.8849 mL

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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

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Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: 2.08 mg/mL (3.92 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (3.92 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Gao Y, et al. Icariside I specifically facilitates ATP or nigericin-induced NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Cell Commun Signal. 2021 Feb 11;19(1):13. [Content Brief]

[2]. Hou M, et al. Icariside I reduces breast cancer proliferation, apoptosis, invasion, and metastasis probably through inhibiting IL-6/STAT3 signaling pathway. J Pharm Pharmacol. 2024 May 3;76(5):499-513. [Content Brief]

[3]. Chen G, et al. Icariside I - A novel inhibitor of the kynurenine-AhR pathway with potential for cancer therapy by blocking tumor immune escape. Biomed Pharmacother. 2022 Sep;153:113387. [Content Brief]

[4]. Chen C, et al. A Novel Prenylflavonoid Icariside I Ameliorates Estrogen Deficiency-Induced Osteoporosis via Simultaneous Regulation of Osteoblast and Osteoclast Differentiation. ACS Pharmacol Transl Sci. 2023 Jan 13;6(2):270-280. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8849 mL	9.4247 mL	18.8494 mL	47.1236 mL
	5 mM	0.3770 mL	1.8849 mL	3.7699 mL	9.4247 mL
	10 mM	0.1885 mL	0.9425 mL	1.8849 mL	4.7124 mL
	15 mM	0.1257 mL	0.6283 mL	1.2566 mL	3.1416 mL
	20 mM	0.0942 mL	0.4712 mL	0.9425 mL	2.3562 mL
	25 mM	0.0754 mL	0.3770 mL	0.7540 mL	1.8849 mL
	30 mM	0.0628 mL	0.3142 mL	0.6283 mL	1.5708 mL
	40 mM	0.0471 mL	0.2356 mL	0.4712 mL	1.1781 mL
	50 mM	0.0377 mL	0.1885 mL	0.3770 mL	0.9425 mL
	60 mM	0.0314 mL	0.1571 mL	0.3142 mL	0.7854 mL
	80 mM	0.0236 mL	0.1178 mL	0.2356 mL	0.5890 mL
	100 mM	0.0188 mL	0.0942 mL	0.1885 mL	0.4712 mL

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Icariside I

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Natural Product Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Glycoside Compound Library

Oxygen Sensing Compound Library

Phenols Library

Pyroptosis Compound Library

Orally Active Compound Library

Traditional Chinese Medicine Active Compound Library

Flavonoids Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Anti-Cancer Natural Product Library

Antidepressant Compound Library

Anti-inflammatory Traditional Chinese Medicine Active Compound Library

Plant-Sourced Natural Product Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Immunopotentiator Compound Library

Anti-Ovarian Cancer Compound Library

Inflammasomes related Compound Library

Multi-Target Compound Library

Radioprotector Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Natural Product Library Plus

Natural Product and Natural Product-Like Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

High-Throughput Natural Product Library

Ancient Chinese Classical Formulas Traditional Chinese Medicine Active Compound Library

Mass Spectrometry Human Metabolite Library

Diarrhea-Related Traditional Chinese Medicine Active Compound Library

Pattern Recognition Receptors Library

High-Efficiency Gene Editing Compound Library

Tonifying Traditional Chinese Medicine Monomer Compound Library

Lactylation Compound Library

Mass Spectrometry Natural Product Library

Publications Citing Use of MedChemExpress (MCE) Icariside I

All NOD-like Receptor (NLR) Isoforms

All STAT Isoforms

All CDK Isoforms

All Bcl-2 Family Isoforms

All JAK Isoforms

All Caspase Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility