KC7F2 | CAS#927822-86-4 | HIF-1 inhibitor

MedKoo Cat#: 407344 | Name: KC7F2

Description:

WARNING: This product is for research use only, not for human or veterinary use.

KC7F2 is a potent HIF-1 pathway inhibitor with potential anticancer activity. KC7F2 is cytotoxic to a variety of cancer cell lines with an IC50 value of 15-25 µM. KC7F2 markedly inhibited HIF-mediated transcription in cells derived from different tumor types, including glioma, breast, and prostate cancers, and exhibited enhanced cytotoxicity under hypoxia. KC7F2 prevented the activation of HIF-target genes such as carbonic anhydrase IX, matrix metalloproteinase 2 (MMP2), endothelin 1, and enolase 1. KC7F2 worked through the down-regulation of HIF-1alpha protein synthesis, an effect accompanied by the suppression of the phosphorylation of eukaryotic translation initiation factor 4E binding protein 1 and p70 S6 kinase, key regulators of HIF-1alpha protein synthesis.

Chemical Structure

KC7F2

CAS#927822-86-4

Theoretical Analysis

MedKoo Cat#: 407344

Name: KC7F2

CAS#: 927822-86-4

Chemical Formula: C16H16Cl4N2O4S4

Exact Mass: 567.8747

Molecular Weight: 570.35

Elemental Analysis: C, 33.69; H, 2.83; Cl, 24.86; N, 4.91; O, 11.22; S, 22.48

Price and Availability

Size	Price	Availability
100mg	USD 450.00	2 Weeks
200mg	USD 650.00	2 Weeks
500mg	USD 1,450.00	2 Weeks
1g	USD 2,050.00	2 Weeks
2g	USD 3,250.00	2 Weeks
5g	USD 4,950.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

KC7F2; KC 7F2; KC-7F2;

IUPAC/Chemical Name

N,N'-(disulfanediylbis(ethane-2,1-diyl))bis(2,5-dichlorobenzenesulfonamide)

InChi Key

REQLACDIZMLXIC-UHFFFAOYSA-N

InChi Code

InChI=1S/C16H16Cl4N2O4S4/c17-11-1-3-13(19)15(9-11)29(23,24)21-5-7-27-28-8-6-22-30(25,26)16-10-12(18)2-4-14(16)20/h1-4,9-10,21-22H,5-8H2

SMILES Code

ClC1=C(S(NCCSSCCNS(C2=C(Cl)C=CC(Cl)=C2)(=O)=O)(=O)=O)C=C(Cl)C=C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

KC7F2 is a potent hypoxia inducible factor-1 (HIF-1) pathway inhibitor with an IC50 of 20 μM in LN229-HRE-AP cells, and with potential as a cancer therapy agent.

In vitro activity:

KC7F2 markedly inhibited HIF-mediated transcription in cells derived from different tumor types, including glioma, breast, and prostate cancers, and exhibited enhanced cytotoxicity under hypoxia. KC7F2 prevented the activation of HIF-target genes such as carbonic anhydrase IX, matrix metalloproteinase 2 (MMP2), endothelin 1, and enolase 1. Reference: Clin Cancer Res. 2009 Oct 1;15(19):6128-36. https://pubmed.ncbi.nlm.nih.gov/19789328/

In vivo activity:

KC7F2 treatment (10 mg/kg/d) in OIR (oxygen-reduced retinopathy) mice significantly attenuated pathological neovascularization and decreased the number of preretinal neovascular cell nuclei, without changing the avascular area, which showed the same trends in OIR rats. Consistently, after the KC7F2 intervention (10 µM), cell proliferation was inhibited in VEGF-induced HUVEC, which was in agreement with the trend observed in the retinas of OIR mice. Reference: Invest Ophthalmol Vis Sci. 2022 Jun 1;63(6):13. https://pubmed.ncbi.nlm.nih.gov/35695808/

	Solvent	mg/mL	mM
Solubility
	DMF	20.0	35.07
	DMF:PBS (pH 7.2) (1:2)	0.3	0.58
	DMSO	50.8	90.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 570.35 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Rathnasamy G, Ling EA, Kaur C. Hypoxia inducible factor-1α mediates iron uptake which induces inflammatory response in amoeboid microglial cells in developing periventricular white matter through MAP kinase pathway. Neuropharmacology. 2014 Feb;77:428-40. doi: 10.1016/j.neuropharm.2013.10.024. Epub 2013 Nov 1. PMID: 24184387. 2. Narita T, Yin S, Gelin CF, Moreno CS, Yepes M, Nicolaou KC, Van Meir EG. Identification of a novel small molecule HIF-1alpha translation inhibitor. Clin Cancer Res. 2009 Oct 1;15(19):6128-36. doi: 10.1158/1078-0432.CCR-08-3180. Epub 2009 Sep 29. PMID: 19789328; PMCID: PMC2770235. 3. Tang X, Cui K, Lu X, Wu P, Yu S, Yang B, Xu Y, Liang X. A Novel Hypoxia-inducible Factor 1α Inhibitor KC7F2 Attenuates Oxygen-induced Retinal Neovascularization. Invest Ophthalmol Vis Sci. 2022 Jun 1;63(6):13. doi: 10.1167/iovs.63.6.13. PMID: 35695808; PMCID: PMC9202333.

In vitro protocol:

In vivo protocol:

1. Tang X, Cui K, Lu X, Wu P, Yu S, Yang B, Xu Y, Liang X. A Novel Hypoxia-inducible Factor 1α Inhibitor KC7F2 Attenuates Oxygen-induced Retinal Neovascularization. Invest Ophthalmol Vis Sci. 2022 Jun 1;63(6):13. doi: 10.1167/iovs.63.6.13. PMID: 35695808; PMCID: PMC9202333.

1: Huang X, He Z, Jiang X, Hou M, Tang Z, Zhen X, Liang Y, Ma J. Folic Acid Represses Hypoxia-Induced Inflammation in THP-1 Cells through Inhibition of the PI3K/Akt/HIF-1α Pathway. PLoS One. 2016 Mar 14;11(3):e0151553. doi: 10.1371/journal.pone.0151553. eCollection 2016. PubMed PMID: 26974319; PubMed Central PMCID: PMC4790958. 2: Cheng CC, Guan SS, Yang HJ, Chang CC, Luo TY, Chang J, Ho AS. Blocking heme oxygenase-1 by zinc protoporphyrin reduces tumor hypoxia-mediated VEGF release and inhibits tumor angiogenesis as a potential therapeutic agent against colorectal cancer. J Biomed Sci. 2016 Jan 28;23:18. doi: 10.1186/s12929-016-0219-6. PubMed PMID: 26822586; PubMed Central PMCID: PMC4730655. 3: Guan G, Zhang Y, Lu Y, Liu L, Shi D, Wen Y, Yang L, Ma Q, Liu T, Zhu X, Qiu X, Zhou Y. The HIF-1α/CXCR4 pathway supports hypoxia-induced metastasis of human osteosarcoma cells. Cancer Lett. 2015 Feb 1;357(1):254-64. doi: 10.1016/j.canlet.2014.11.034. Epub 2014 Nov 18. PubMed PMID: 25444927. 4: Li J, Jiang G, Chen Y, Chen L, Li Z, Wang Z, Wang X. Altered expression of hypoxia-Inducible factor-1α participates in the epileptogenesis in animal models. Synapse. 2014 Sep;68(9):402-9. doi: 10.1002/syn.21752. Epub 2014 Jun 17. PubMed PMID: 24889205. 5: Rathnasamy G, Ling EA, Kaur C. Hypoxia inducible factor-1α mediates iron uptake which induces inflammatory response in amoeboid microglial cells in developing periventricular white matter through MAP kinase pathway. Neuropharmacology. 2014 Feb;77:428-40. doi: 10.1016/j.neuropharm.2013.10.024. Epub 2013 Nov 1. PubMed PMID: 24184387. 6: Narita T, Yin S, Gelin CF, Moreno CS, Yepes M, Nicolaou KC, Van Meir EG. Identification of a novel small molecule HIF-1alpha translation inhibitor. Clin Cancer Res. 2009 Oct 1;15(19):6128-36. doi: 10.1158/1078-0432.CCR-08-3180. Epub 2009 Sep 29. PubMed PMID: 19789328; PubMed Central PMCID: PMC2770235. 7: Koh MY, Spivak-Kroizman TR, Powis G. Inhibiting the hypoxia response for cancer therapy: the new kid on the block. Clin Cancer Res. 2009 Oct 1;15(19):5945-6. doi: 10.1158/1078-0432.CCR-09-1650. Epub 2009 Sep 29. PubMed PMID: 19789327; PubMed Central PMCID: PMC2760048.