2. Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Stem Cell/Wnt JAK/STAT Signaling Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK Epigenetics
  3. Apoptosis Reactive Oxygen Species (ROS) NOD-like Receptor (NLR) STAT CDK Bcl-2 Family Aryl Hydrocarbon Receptor JAK Caspase IFNAR PD-1/PD-L1
  4. Icariside I

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.

Icariside I

Icariside I Chemical Structure

CAS No. : 56725-99-6

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

Other Forms of Icariside I:

Icariside I Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Icariside I

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NLRP3 NLRP1 NOD1 NOD2

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STAT3 STAT5 STAT6 STAT1

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

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JAK1 JAK2 JAK3 Tyk2 JAK

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4].

IC50 & Target[1]

NLRP3

 

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.

Icariside I Related Antibodies

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.
Molecular Weight

530.52

Formula

C27H30O11
CAS No.
Appearance

Solid

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
Structure Classification
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)

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8849 mL 9.4247 mL 18.8494 mL
5 mM 0.3770 mL 1.8849 mL 3.7699 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 (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.

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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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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: 2.08 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.

    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: 2.08 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.

    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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mg/kg

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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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% 
+
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%
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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 (sealed storage, away from moisture and 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: 99.30%

SDS (393 KB)

COA (250 KB) HNMR (152 KB) CNMR (133 KB) RP-HPLC (208 KB) MS (418 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 (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.

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 Related Classifications

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  • 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:

Icariside I56725-99-6Icarisid IApoptosisReactive Oxygen Species (ROS)NOD-like Receptor (NLR)STATCDKBcl-2 FamilyAryl Hydrocarbon ReceptorJAKCaspaseIFNARPD-1/PD-L1Cyclin dependent kinaseAhRJanus kinaseInterferon-α/β receptorInterferon-alpha/beta receptor PD-1/Programmed death-ligand 1BMDMsBMMsIDILI4T1-luc cellsOVXosteoporosis mouseInhibitorinhibitorinhibit

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