ITSA-1 (ITSA1)
目录号 : GC14597
ITSA-1 (ITSA1)是一种组蛋白去乙酰化酶（HDAC）激活剂，可以防止动脉层流剪切力诱导的内皮细胞脱落，并降低血管内皮细胞（vECs）中VCAM-1的表达。
Cas No.:200626-61-5
Sample solution is provided at 25 µL, 10mM.
ITSA-1 (ITSA1), a histone deacetylase (HDAC) activator, can prevent arterial laminar shear stress-induced endothelial cell detachment and reduce VCAM-1 expression in vascular endothelial cells (vECs)[1].
In vitro, ITSA-1 (150μM; 0, 3, 6; 24h) can reverse the inflammatory response in vascular endothelial cells (vECs) induced by amyotrophic lateral sclerosis (ALS) by increasing the expression of histone deacetylases (HDACs) and histone H3 lysine 9 trimethylation (H3K9me3)[2]. Short-term stimulation with ITSA-1 (0, 50, 100, 200 and 400ng/ml; 0, 24 and 48h) induces epithelial-mesenchymal transition in nasopharyngeal carcinoma cells[3].
In vivo, ITSA-1 (0.5mg/kg; i.p.) enhances the recovery and survival of post-ROSC rats by diminishing histone acetylation and mitigating systemic inflammation[1]. A blockade of HDAC3 inhibition in CBS+/− mice by HDAC activator ITSA-1 (0.5mg/kg/3 times/week; 8 weeks; i.p.), led to the remodeling of histone landscapes in the genome and thereby attenuated histone acetylation-dependent inflammatory signaling[4].
References:
[1] Zhang C, Wei H, Zhang Q, et al. The Histone Deacetylase Activator ITSA-1 Improves the Prognosis of Cardiac Arrest Rats by Alleviating Systemic Inflammatory Responses Following Cardiopulmonary Resuscitation. Mediators Inflamm. 2025 Mar 20;2025:8156593.
[2] Wang TY, Chang MM, Li YJ, et al. Maintenance of HDACs and H3K9me3 Prevents Arterial Flow-Induced Venous Endothelial Damage. Front Cell Dev Biol. 2021 Apr 9;9:642150.
[3] Shen Z, Liao X, Shao Z, et al. Short-term stimulation with histone deacetylase inhibitor trichostatin a induces epithelial-mesenchymal transition in nasopharyngeal carcinoma cells without increasing cell invasion ability. BMC Cancer. 2019 Mar 22;19(1):262.
[4] Behera J, Kelly KE, Voor MJ, et al. Hydrogen Sulfide Promotes Bone Homeostasis by Balancing Inflammatory Cytokine Signaling in CBS-Deficient Mice through an Epigenetic Mechanism. Sci Rep. 2018 Oct 15;8(1):15226.
ITSA-1 (ITSA1)是一种组蛋白去乙酰化酶（HDAC）激活剂，可以防止动脉层流剪切力诱导的内皮细胞脱落，并降低血管内皮细胞（vECs）中VCAM-1的表达[1]。
体外实验中，ITSA-1（150µM; 0, 3, 6和24小时）可以通过增加组蛋白去乙酰化酶（HDACs）和组蛋白H3第9位赖氨酸三甲基化（H3K9me3）的表达，逆转由肌萎缩侧索硬化症（ALS）诱导的血管内皮细胞（vECs）的炎症反应[2]。短期刺激ITSA-1（0, 50, 100, 200和400ng/ml; 0, 24和48小时）可以诱导鼻咽癌细胞发生上皮-间充质转化[3]。
体内实验中，ITSA-1（0.5mg/kg; 腹腔注射）通过减少组蛋白乙酰化和减轻全身炎症反应，增强了心脏骤停后复苏（post-ROSC）大鼠的恢复和存活率[1]。通过组蛋白去乙酰化酶激活剂ITSA-1（0.5mg/kg/每周3次; 8周; 腹腔注射）阻断CBS+/−小鼠中HDAC3的抑制，导致基因组中组蛋白景观的重塑，从而减轻了依赖组蛋白乙酰化的炎症信号传导[4]。
| Cell experiment [1]: | |
Cell lines | CNE2 and C666-1 cells |
Preparation Method | CNE2 and C666-1 cells were treated with 0 and 200ng/ml ITSA-1 for 0, 24 and 48h, and then cells were photographed under inverted microscope. CNE2 and C666-1 cells were treated with various concentrations of ITSA-1 (0, 50, 100, 200 and 400ng/ml) for short period within 48h, and then cells were harvested and subjected to real-time PCR and western blot analysis of EMT-associated E-cadherin, Vimentin, Snail1 and Twist1 gene and protein expressions. |
Reaction Conditions | 0, 50, 100, 200 and 400ng/ml; 0, 24 and 48h |
Applications | Short-term stimulation with ITSA-1 induces epithelial-mesenchymal transition in nasopharyngeal carcinoma cells. |
| Animal experiment [2]: | |
Animal models | Adult male Wistar rats |
Preparation Method | All rats were randomly divided into five groups: Normal group: The rats received the same treatment as the other groups except that they did not undergo cardiac arrest (CA) and cardiopulmonary resuscitation (CPR), until the end of the operation. Sham group: Rats were subjected to mechanical ventilation while Vecuronium bromide was administered. Control group, Suberoylanilide hydroxamic acid (SAHA) group, and ITSA-1 group: Rats in these groups were administered normal saline, SAHA, or ITSA-1 via intraperitoneal injection at a dose of 100mg/kg or 0.5mg/kg. These injections were given per kilogram of body weight for three consecutive days before the asphyxiated CA surgery. Experiment 1 (n=45): Five rats each in the normal and sham groups and 10 each in the control, SAHA, and ITSA-1 groups were used to investigate the effects of the drug on cardiac function 4h after post-CA syndrome (ROSC). Additionally, survival status and neurological function, including the neurological deficit score (NDS) at 24, 48, and 72h after ROSC, and performance in the Morris water maze at 72h after ROSC, were assessed. Experiment 2 (n=24): Three rats each in the normal and sham groups and five each in the control, SAHA, and ITSA-1 groups were used to observe the effects of ITSA-1 on the levels of TNF-α, IL-1β, glial fibrillary acidic protein (GFAP), and S100β in plasma, as well as TNF-α and IL-1β levels in the hippocampus 4h after CA-ROSC. This experiment also aimed to evaluate the effect of ITSA-1 on the infiltration of astrocytes and microglia in the hippocampus 4h after ROSC. |
Dosage form | 0.5mg/kg; i.p. |
Applications | ITSA-1 enhances the recovery and survival of post-ROSC rats by diminishing histone acetylation and mitigating systemic inflammation. |
References: | |
| Cas No. | 200626-61-5 | SDF | |
| 化学名 | (1H-benzo[d][1,2,3]triazol-1-yl)(2,4-dichlorophenyl)methanone | ||
| Canonical SMILES | O=C(N1N=NC2=CC=CC=C21)C3=CC=C(Cl)C=C3Cl | ||
| 分子式 | C13H7Cl2N3O | 分子量 | 292.12 |
| 溶解度 | ≥ 89mg/mL in DMSO | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4233 mL | 17.1163 mL | 34.2325 mL |
| 5 mM | 0.6847 mL | 3.4233 mL | 6.8465 mL |
| 10 mM | 0.3423 mL | 1.7116 mL | 3.4233 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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- Purity: >98.00%
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