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

Product Specifications

CAS Number

[56725-99-6]

Product Name Alternative

Icarisid I

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Aryl Hydrocarbon Receptor; Bcl-2 Family; Caspase; CDK; IFNAR; JAK; NOD-like Receptor (NLR) ; PD-1/PD-L1; Reactive Oxygen Species (ROS) ; STAT

Type

Natural Products

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; Immunology/Inflammation; JAK/STAT Signaling; Metabolic Enzyme/Protease; NF-κB; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Field of Research

Cancer; Endocrinology; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/Icariside_I.html

Purity

99.30

Solubility

DMSO : 62.5 mg/mL (ultrasonic)

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

Molecular Formula

C27H30O11

Molecular Weight

530.52

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.|[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.|[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.