Icariside I (Standard)

Icariside I (Standard) is the analytical standard of Icariside I (HY-N1939). This product is intended for research and analytical applications. 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]. 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].
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].