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Ionomycin free acid Sale

(Synonyms: 离子霉素,SQ23377) 目录号 : GC15446

Ionomycin free acid 是一种选择性的强效钙离子载体,可作为活性 Ca2+ 载体。

Ionomycin free acid Chemical Structure

Cas No.:56092-81-0

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1mg
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Description

Ionomycin free acid is a selective and potent calcium ion carrier that acts as an active Ca2+ carrier. By stimulating the entry of storage-regulated cations across biofilms, effectively improves Ca2+ influx[9].

Human NK cells treated with Ionomycin free acid lose their ability to degranulate and secrete IFN-γ in response to a variety of stimuli, but IL-2 stimulation can compensate these defects[2]. When tested hypothesis by hyperpolarizing HL-60 cells using Ionomycin free acid before electroporation. Hyperpolarizing cells before electroporation alters the pulsed electric field intensity thresholds for reversible electroporation and IRE, allowing for greater control and selectivity of electroporation outcomes[3]. Ionomycin free acid induces calcium influx into the intracellular region and reactive oxygen species production in N1E-115 cells. Lipid hydroperoxide production was induced in ionomycin-treated N1E-115 cells[5]. Ionomycin free acid, at least in part, exerts its effects via specific binding to a G-protein coupled receptor, thereby evoking downstream cellular events like arachidonate release with subsequent prostaglandin formation[6]. A high concentration of Ionomycin free acid increased the frequency and amplitude of calcium oscillation patterns, affecting the balance of mitochondrial energy metabolism, leading to increased reactive oxygen species (ROS) and decreased ATP[1].

Intratumoral injection of Ionomycin free acid into subcutaneous HT1376 tumors reduced the tumorigenicity in nude mice. Furthermore, these in vivo growth-inhibitory effects of Ionomycin free acid were significantly enhanced by pretreatment with cisplatin[8]. Acetylcholine (ACh) evoked secretion by the calcium ionophore, ionomycin, was studied at frog motor nerve endings. Bath application of Ionomycin free acid stimulated an irreversible increase in the rate of spontaneous, quantal ACh release in the presence of extracellular Ca2+. In contrast, local application of Ionomycin free acid stimulated a rapid, reversible acceleration of spontaneous ACh release[4]. Following stimulation with Ionomycin free acid, PD-1+ICOS+ CD4+ T cells expressed significantly lower IL-17A, but not IFNγ, levels in GF BXD2 mice compared to SPF BXD2 mice[7].

References:
[1]. Chen C, Sun T, et,al. Ionomycin-induced mouse oocyte activation can disrupt preimplantation embryo development through increased reactive oxygen species reaction and DNA damage. Mol Hum Reprod. 2020 Oct 1;26(10):773-783. doi: 10.1093/molehr/gaaa056. PMID: 32697831.
[2]. Romera-Cárdenas G, Thomas LM, et,al. Ionomycin Treatment Renders NK Cells Hyporesponsive. PLoS One. 2016 Mar 23;11(3):e0150998. doi: 10.1371/journal.pone.0150998. PMID: 27007115; PMCID: PMC4805247.
[3]. Aiken EJ, Kilberg BG, et,al. Ionomycin-Induced Changes in Membrane Potential Alter Electroporation Outcomes in HL-60 Cells. Biophys J. 2018 Jun 19;114(12):2875-2886. doi: 10.1016/j.bpj.2018.05.018. PMID: 29925024; PMCID: PMC6026377.
[4]. Hunt JM, Silinsky EM. Ionomycin-induced acetylcholine release and its inhibition by adenosine at frog motor nerve endings. Br J Pharmacol. 1993 Oct;110(2):828-32. doi: 10.1111/j.1476-5381.1993.tb13887.x. PMID: 8242258; PMCID: PMC2175912.
[5]. Nakamura S, Nakanishi A, et,al. Ionomycin-induced calcium influx induces neurite degeneration in mouse neuroblastoma cells: analysis of a time-lapse live cell imaging system. Free Radic Res. 2016;50(11):1214-1225. doi: 10.1080/10715762.2016.1227074. Epub 2016 Sep 29. PMID: 27573976.
[6]. Leis HJ, Windischhofer W. Ionomycin induces prostaglandin E2 formation in murine osteoblastic MC3T3-E1 cells via mechanisms independent of its ionophoric nature. Biochem Cell Biol. 2016 Jun;94(3):236-40. doi: 10.1139/bcb-2015-0148. Epub 2016 Feb 9. PMID: 27065246.
[7]. Hong H, Alduraibi F, et,al. Host Genetics But Not Commensal Microbiota Determines the Initial Development of Systemic Autoimmune Disease in BXD2 Mice. Arthritis Rheumatol. 2022 Apr;74(4):634-640. doi: 10.1002/art.42008. Epub 2022 Feb 10. PMID: 34725967; PMCID: PMC9071869.
[8]. Miyake H, Hara I, et,al. Calcium ionophore, ionomycin inhibits growth of human bladder cancer cells both in vitro and in vivo with alteration of Bcl-2 and Bax expression levels. J Urol. 1999 Sep;162(3 Pt 1):916-21. doi: 10.1097/00005392-199909010-00090. PMID: 10458408.
[9]. Erdahl WL, Chapman CJ, et,al. Ionomycin, a carboxylic acid ionophore, transports Pb(2+) with high selectivity. J Biol Chem. 2000 Mar 10;275(10):7071-9. doi: 10.1074/jbc.275.10.7071. PMID: 10702273.

Ionomycin free acid 是一种选择性的强效钙离子载体,可作为活性 Ca2+ 载体。通过刺激存储调节阳离子进入生物膜,有效提高 Ca2+ 内流[9]

用离子霉素游离酸处理的人 NK 细胞失去脱颗粒和分泌 IFN-γ 的能力以响应各种刺激,但 IL-2 刺激可以弥补这些缺陷[2]。当通过在电穿孔前使用离子霉素游离酸使 HL-60 细胞超极化来检验假设时。电穿孔前超极化细胞会改变可逆电穿孔和 IRE 的脉冲电场强度阈值,从而更好地控制和选择性电穿孔结果[3]。 Ionomycin free acid 在 N1E-115 细胞中诱导钙流入细胞内区域并产生活性氧。在离子霉素处理的 N1E-115 细胞中诱导脂质氢过氧化物的产生[5]。离子霉素游离酸至少部分通过与 G 蛋白偶联受体特异性结合发挥作用,从而引发下游细胞事件,如花生四烯酸释放以及随后的前列腺素形成[6]。高浓度的离子霉素游离酸增加钙振荡模式的频率和幅度,影响线粒体能量代谢的平衡,导致活性氧(ROS)增加和ATP减少[1]。p>\n

将离子霉素游离酸瘤内注射到皮下 HT1376 肿瘤中可降低裸鼠的致瘤性。此外,通过顺铂预处理显着增强了离子霉素游离酸的这些体内生长抑制作用[8]。在青蛙运动神经末梢研究了乙酰胆碱 (ACh) 引起的钙离子载体、离子霉素的分泌。在细胞外 Ca2+ 存在的情况下,离子霉素游离酸的浴应用刺激了自发的、量子 ACh 释放速率的不可逆增加。相比之下,局部应用离子霉素游离酸可刺激 ACh 自发释放的快速、可逆加速[4]。与 SPF BXD2 小鼠相比,用离子霉素游离酸刺激后,PD-1+ICOS+ CD4+ T 细胞表达的 IL-17A 水平显着低于 SPF BXD2 小鼠[7]

实验参考方法

Cell experiment [1]:

Cell lines

NK cell

Preparation Method

Cells were then treated with either 1 µM Ionomycin free acid or DMSO, as vehicle control, and cultured for 16 hours. Control and ionomycin-treated cells were then washed and allowed to rest for 24 hours at 2x106 cells/mL in RPMI 10% FBS.

Reaction Conditions

1 µM Ionomycin free acid for 16 hours

Applications

Human NK cells treated with Ionomycin free acid lose their ability to degranulate and secrete IFN-γ in response to a variety of stimuli, but IL-2 stimulation can compensate these defects.

Animal experiment [2]:

Animal models

Athymic nude mice (Balb/c nu/nu female, 6 to 8 weeks old)

Preparation Method

The effects of intratumoral injection of Ionomycin free acid on the growth of subcutaneous HT1376 tumors established in athymic nude mice were then tested.

Dosage form

Intratumoral injection 100 ug Ionomycin free acid 3 times a week for 4 weeks

Applications

Intratumoral injection of Ionomycin free acid into subcutaneous HT1376 tumors reduced the tumorigenicity in nude mice.

References:

[1].Romera-CÁrdenas G, Thomas LM, et,al. Ionomycin Treatment Renders NK Cells Hyporesponsive. PLoS One. 2016 Mar 23;11(3):e0150998. doi: 10.1371/journal.pone.0150998. PMID: 27007115; PMCID: PMC4805247.
[2]. Miyake H, Hara I, et,al. Calcium ionophore, ionomycin inhibits growth of human bladder cancer cells both in vitro and in vivo with alteration of Bcl-2 and Bax expression levels. J Urol. 1999 Sep;162(3 Pt 1):916-21. doi: 10.1097/00005392-199909010-00090. PMID: 10458408.

化学性质

Cas No. 56092-81-0 SDF
别名 离子霉素,SQ23377
化学名 (4R,6R,8R,10E,12S,14S,16E,18S,19S,20R,21S)-11,19,21-trihydroxy-22-((2R,2'R,5R,5'R)-5'-((R)-1-hydroxyethyl)-2,5'-dimethyloctahydro-[2,2'-bifuran]-5-yl)-4,6,8,12,14,18,20-heptamethyl-9-oxodocosa-10,16-dienoic acid
Canonical SMILES O[C@H](C)[C@]1(C)O[C@H](CC1)[C@]2(C)O[C@@H](C[C@@H]([C@@H](C)[C@H]([C@H](/C=C/C[C@H](C)C[C@H](C)/C(O)=C\C([C@H](C)C[C@H](C)C[C@H](C)CCC(O)=O)=O)C)O)O)CC2
分子式 C41H72O9 分子量 709.01
溶解度 1.4mg/mL in DMSO, 2.5mg/mL in DMF 储存条件 Desiccate at -20°C
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