KC7F2
KC7F2 is a novel inhibitor of HIF-1αwith IC50 value of 20 μM [1].
Hypoxia inducible factor-1 (HIF-1) is a heterodimeric transcription factor consisting of α and β subunits. In normal situation, the HIF-1α subunit is constitutively translated, but rapidly degraded. While, under hypoxia it is stabilized. HIF target genes encode a series of critical factors to adapt the low oxygen [1].
In a HIF-reporter cell line LN229-HRE-AP, KC7F2 (>25 μM) reduced AP activity by 90% in LN229 cells, which indicated that KC7F2 inhibited AP enzyme activity. In LNZ308 human glioma cells, KC7F2 inhibited the expression of a panel of HIF target genes, such as matrix metalloproteinase 2 (MMP2), enolase 1, carbonic anhydrase IX (CA IX) and endothelin 1. Also, KC7F2 reduced expression of HIF-1α in a dose-dependent way [1].
In a rat epilepsy model, KC7F2 significantly shortened the latent period in the PTZ kindling model and increased the rate of spontaneous recurrent seizures during the chronic stage in the lithium-pilocarpine model [3].
References:
[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. Nimmy Varghese, Amandine Grimm, et al. "From Young to Old: Mimicking Neuronal Aging in Directly Converted Neurons from Young Donors." Cells. 2024 Jul 26;13(15):1260 PMID: 39120291
- 2. Nimmy Varghese, Leonora Szabo, et al. "Preservation of an Aging-Associated Mitochondrial Signature in Advanced Human Neuronal Models." bioRxiv. March 31, 2024.
- 3. Zheng Peng, Xiao-Jian Li, et al. "Hydrogen inhalation therapy regulates lactic acid metabolism following subarachnoid hemorrhage through the HIF-1α pathway." Biochem Biophys Res Commun. 2023 Jun 30:663:192-201. PMID: 37141668
- 4. 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
- 5. 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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
U251MG (glioma), PC3 (prostate cancer), MCF7 (breast cancer), and LNZ308 (glioblastoma) cell lines |
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Reaction Conditions |
40 μmol/L KC7F2 for 8 or 24 h incubation |
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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] | |
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Animal models |
Male Sprague-Dawley rats, 210 ~ 250 g |
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Dosage form |
2 mg/ml Administered via an intracerebroventricular microinjection (i.c.v) into the brain |
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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. |
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Note |
The technical data provided above is for reference only. |
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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. |
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