HO-1-IN-1 hydrochloride
目录号 : GC34618
HO-1-IN-1 hydrochloride是一种血红素氧合酶-1（HO-1）抑制剂，其IC50为 0.25μM[1。
Cas No.:1092851-70-1
Sample solution is provided at 25 µL, 10mM.
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HO-1-IN-1 hydrochloride is a heme oxygenase 1 (HO-1) inhibitor with an IC50 of 0.25μM[1]. HO-1 is an inducible enzyme that plays a key role in maintaining cellular redox balance and protecting cells from oxidative stress by catalyzing the degradation of heme to produce carbon monoxide, biliverdin, and free iron[2][3]. HO-1-IN-1 hydrochloride is usually used in studies related to oxidative stress, inflammatory responses, and apoptosis[4][5].
In vitro, HO-1-IN-1 hydrochloride (10μM; 4h) attenuated GRIM-19 deficiency-induced NF-κB activation and p65 nuclear translocation in GES-1 cells[6]. HO-1-IN-1 hydrochloride (5-10μM; 6h) significantly attenuated GRIM-19 deficiency-driven gastric cancer cell migration and invasion, and downregulated metastasis-associated gene expressions such as HIF-1α, COX-2, VEGF-A, VEGF-C, MMP-9, and BACH-1[7].
References:
[1] Floresta G, Pittalà V, Sorrenti V, Romeo G, Salerno L, Rescifina A. Development of new HO-1 inhibitors by a thorough scaffold-hopping analysis. Bioorg Chem. 2018;81:334-339.
[2] Consoli V, Sorrenti V, Grosso S, Vanella L. Heme Oxygenase-1 Signaling and Redox Homeostasis in Physiopathological Conditions. Biomolecules. 2021;11(4):589.
[3] Ryter SW. Heme oxygenase-1/carbon monoxide as modulators of autophagy and inflammation. Arch Biochem Biophys. 2019;678:108186.
[4] Lu JJ, Abudukeyoumu A, Zhang X, Liu LB, Li MQ, Xie F. Heme oxygenase 1: a novel oncogene in multiple gynecological cancers. Int J Biol Sci. 2021;17(9):2252-2261.
[5] Spampinato M, Sferrazzo G, Pittalà V, et al. Non-competitive heme oxygenase-1 activity inhibitor reduces non-small cell lung cancer glutathione content and regulates cell proliferation. Mol Biol Rep. 2020;47(3):1949-1964.
[6] Zeng X, Yang M, Ye T, et al. Mitochondrial GRIM-19 loss in parietal cells promotes spasmolytic polypeptide-expressing metaplasia through NLR family pyrin domain-containing 3 (NLRP3)-mediated IL-33 activation via a reactive oxygen species (ROS) -NRF2- Heme oxygenase-1(HO-1)-NF-кB axis. Free Radic Biol Med. 2023;202:46-61.
[7] Wang X, Ye T, Xue B, et al. Mitochondrial GRIM-19 deficiency facilitates gastric cancer metastasis through oncogenic ROS-NRF2-HO-1 axis via a NRF2-HO-1 loop. Gastric Cancer. 2021;24(1):117-132.
HO-1-IN-1 hydrochloride是一种血红素氧合酶-1（HO-1）抑制剂，其IC50为 0.25μM[1。HO-1是一种可诱导酶，通过催化血红素降解产生一氧化碳、胆绿素和游离铁，从而在维持细胞氧化还原平衡和保护细胞免受氧化应激方面发挥关键作用[2][3]。HO-1-IN-1 hydrochloride 通常用于氧化应激、炎症反应和凋亡相关研究[4][5]。
在体外实验中，HO-1-IN-1 hydrochloride（10μM；4小时）可减轻GRIM-19缺陷诱导的GES-1细胞中NF-κB激活和p65核转位[6]。此外，HO-1-IN-1 hydrochloride（5-10μM；6小时）显著抑制GRIM-19缺陷驱动的胃癌细胞迁移和侵袭，并下调HIF-1α、COX-2、VEGF-A、VEGF-C、MMP-9和BACH-1等与肿瘤转移相关的基因表达[7]。
| Cell experiment [1]: | |
Cell lines | Human normal gastric epithelial GES-1 cells |
Preparation Method | Human normal gastric epithelial GES-1 cells were cultured in DMEM or RPMI 1640 supplemented with 10% fetal bovine serum, 100U/ml penicillin and 100μg/ml streptomycin at 37℃ in a humidified chamber containing 5% CO2. Recombinant CRISPR/Cas9 lentivirus harboring GRIM-19-specific small-guide RNA 134 target (sgRNA-134) and corresponding negative control (NC) with GFP reporter gene were constructed. GES-1 cells at 60% confluence were infected with a multiplicity of infection (MOI) at 30 and 50, respectively. The infected GFP+cells were sorted by flow cytometry and single-cell clones were screened and expanded in vitro. GRIM-19 expression was determined by western blotting and IF staining. GRIM-19-deficient GES-1 cells were treated with HO-1-IN-1 hydrochloride (10μM) for 4h. NF-кB transcriptional activation was analyzed by luciferase reporter assay, while p65, p-p65 and NF-кB downstream targets were detected by western blotting. |
Reaction Conditions | 10μM; 4h |
Applications | HO-1-IN-1 hydrochloride attenuated GRIM-19 deficiency-induced NF-κB activation and p65 nuclear translocation in GES-1 cells. |
References: | |
| Cas No. | 1092851-70-1 | SDF | |
| Canonical SMILES | BrC1=CC=C(CCCCN2C=CN=C2)C=C1.Cl | ||
| 分子式 | C13H16BrClN2 | 分子量 | 315.64 |
| 溶解度 | DMSO : 125 mg/mL (396.02 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1682 mL | 15.8408 mL | 31.6817 mL |
| 5 mM | 633.6 μL | 3.1682 mL | 6.3363 mL |
| 10 mM | 316.8 μL | 1.5841 mL | 3.1682 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet