KC7F2

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KC7F2

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

927822-86-4

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
10mg	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	570.38
Cas No.	927822-86-4
Formula	C₁₆H₁₆Cl₄N₂O₄S₄
Solubility	≥24.95 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
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	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。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。

资料参考

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.

试验操作

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.