KC7F2
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
KC7F2是HIF-1α的一个新型抑制剂，IC50值20 μM[1]。
低氧诱导因子1(HIF-1)是一个由α和β亚基组成的异质二聚体转录因子。在正常情况下，HIF-1α亚基的翻译是组成性的，然而会迅速降解。同时，在低氧情况下它是稳定的。HIF目标基因编码一系列关键因子来适应低氧[1]。
在HIF受体细胞系LN229-HRE-AP中，KC7F2 (> 25μM)减少了LN229细胞中AP活性的90%，这表明KC7F2抑制了AP酶活性。在LNZ308人神经胶质瘤细胞中，KC7F2抑制一组HIF目标基因的表达，如基质金属蛋白酶2(MMP2)、烯醇酶1、第九碳酸酐酶IX(CA IX)和内皮素1。KC7F2也可以剂量依赖的方式减少HIF-1α的表达[1]。
参考文献：
[1]. Narita T, Yin S, Gelin CF, et al. Identification of a novel small molecule HIF-1alpha translation inhibitor. Clin Cancer Res, 2009, 15(19): 6128 - 6136.
[2]. Li J, Jiang G, Chen Y, et al. Altered expression of hypoxia-Inducible factor-1α participates in the epileptogenesis in animal models. Synapse, 2014, 68(9): 402 - 409.
- 1. Na Jiang, Hao Zhao, et al. "HIF‐1α ameliorates tubular injury in diabetic nephropathy via HO‐1–mediated control of mitochondrial dynamics." Cell Prolif. 2020 Nov;53(11):e12909. PMID:32975326
- 2. Chen Z, Tian D, et al. "Apigenin Combined With Gefitinib Blocks Autophagy Flux and Induces Apoptotic Cell Death Through Inhibition of HIF-1α, c-Myc, p-EGFR, and Glucose Metabolism in EGFR L858R+T790M-Mutated H1975 Cells." Front Pharmacol. 2019 Mar 22;10:260. PMID:30967777
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 570.38 |
| Cas No. | 927822-86-4 |
| Formula | C16H16Cl4N2O4S4 |
| Solubility | ≥137.4 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | 2,5-dichloro-N-[2-[2-[(2,5-dichlorophenyl)sulfonylamino]ethyldisulfanyl]ethyl]benzenesulfonamide |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=C(C=C1Cl)S(=O)(=O)NCCSSCCNS(=O)(=O)C2=C(C=CC(=C2)Cl)Cl)Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Cell experiment:[1] | |
|
Cell lines |
U251MG (glioma), PC3 (prostate cancer), MCF7 (breast cancer), and LNZ308 (glioblastoma) cell lines |
|
Reaction Conditions |
40 μmol/L KC7F2 for 8 or 24 h incubation |
|
Applications |
KC7F2 markedly inhibited hypoxia inducible factor-1 (HIF-1)-mediated transcription in cells derived from different tumor types, including glioma, breast, and prostate cancers, and exhibited enhanced cytotoxicity under hypoxia. In LNZ308 human glioma cells grown under hypoxic conditions, KC7F2 was also proved to prevent the activation of HIF-1 target genes such as carbonic anhydrase IX, matrix metalloproteinase 2, endothelin 1, and enolase 1. |
| Animal experiment:[2] | |
|
Animal models |
Male Sprague-Dawley rats, 210 ~ 250 g |
|
Dosage form |
2 mg/ml Administered via an intracerebroventricular microinjection (i.c.v) into the brain |
|
Applications |
KC7F2 significantly shortened the latent period in pentylenetetrazole (PTZ) chronic kindling model and increased the rate of spontaneous recurrent seizures during the chronic stage of the lithium-pilocarpine epilepsy model. Thus, HIF-1α inhibitor KC7F2 could be used to detect changes in the animal behavior in PTZ and lithium-pilocarpine epilepsy models. |
|
Note |
The technical data provided above is for reference only. |
|
References: 1. Narita T, Yin S, Gelin CF, et al. Identification of a novel small molecule HIF-1alpha translation inhibitor. Clinical Cancer Research, 2009, 15(19): 6128-6136. 2. Li J, Jiang G, Chen Y, et al. Altered expression of hypoxia-Inducible factor-1α participates in the epileptogenesis in animal models. Synapse, 2014, 68(9): 402-409. |
|
质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
