Hypoxia inducible factor-1α inhibitor InhibitorAn HIF and HIF-1α inhibitor which suppresses expression of downstream target genes

Hypoxia inducible factor-1α inhibitor Inhibitor (CAS 934593-90-5)

Hypoxia inducible factor-1α Inhibitor | CAS 934593-90-5 is rated 5.0 out of 5 by 1.
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Synonym: methyl 3-[[2-[4-(2-adamantyl)phenoxy]acetyl]amino]-4-hydroxybenzoate; HIF-1 Inhibitor
Application: An HIF and HIF-1α inhibitor which suppresses expression of downstream target genes
CAS Number: 934593-90-5
Purity: ≥97%
Molecular Weight: 435.51
Molecular Formula: C26H29NO5
* Refer to Certificate of Analysis for lot specific data (including water content).
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Hypoxia Inducible Factor-1α Inhibitor is a novel small molecule which inhibits HIF by reducing HIF-1α accumulation and gene transcriptional activity. In a gene reporter assay using human AGS and Hep3B cell lines, hypoxia inducible factor-1α Inhibitor prevented HIF-1 transcriptional activity with IC50 values of 2.6 and 0.7 μM, respectively. Hypoxia inducible factor-1α inhibitor blocks HIF-1α accumulation in Hep3B cells in a concentration and time-dependent manner, with complete inhibition at a concentration of 30 μM within 12 hours. Hypoxia inducible factor-1α inhibitor also significantly suppresses transcription of the HIF-1 target genes VEGF and erythropoietin at 10 μM.


References

1 Wang, G.L., Jiang, B., Rue, E.A., et al. Hypoxia-inducible factor 1 is a basic-helix-loop-helix-PAS heterodimer regulated by cellular O2 tension. Proc Natl Acad Sci USA 92 5510-5514 (1995). 2 Safran, M., Kaelin, W.G. HIF hydroxylation and the mammalian oxygen-sensing pathway. J Clin Invest 111 779-783 (2003). 3 Lee, K., Lee, J.H., Boovanahalli, S.K., et al. (Aryloxyacetylamino)benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors. J Med Chem 50 1675-1684 (2007).

Physical State :
Solid
Solubility :
Soluble in DMF (~10 mg/ml), and DMSO (~10 mg/ml). Insoluble in water(25° C).
Storage :
Store at -20° C
Boiling Point :
655.48° C at 760 mmHg (Predicted)
Density :
1.28 g/cm3 (Predicted)
Refractive Index :
n20D 1.63 (Predicted)
IC50 :
HIF-1 transcriptional activity: IC50 = 0.7 µM (human Hep3B cell lines); HIF-1 transcriptional activity: IC50 = 2.6 µM (human AGS cell lines)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
35028748
MDL Number :
MFCD09907563
SMILES :
COC(=O)C1=CC(=C(C=C1)O)NC(=O)COC2=CC=C(C=C2)C3C4CC5CC(C4)CC3C5

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Certificate of Analysis

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Hypoxia inducible factor-1α inhibitor Inhibitor  Product Citations

See how others have used Hypoxia inducible factor-1α inhibitor Inhibitor. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 14 total

PMID: # 30854715  Patra, K.|Jana, S.|Sarkar, A.|Mandal, DP.|Bhattacharjee, S.| et al. 2019. Biofactors. 45: 401-415.

PMID: # 29396728  Wilkes, JG. et al. 2018. Clin. Exp. Metastasis. 35: 37-51.

PMID: # 29030976  Chen, YF. et al. 2017. J. Cell. Physiol.

PMID: # 27805282  Matijevic Glavan, T. et al. 2017. Mol. Carcinog. 56: 1214-1226.

PMID: # 28446589  Yamazaki, R. et al. 2017. FASEB J. 31: 3359-3371.

PMID: # 27750035  Galardo, MN. et al. 2017. Biochimie. 132: 9-18.

PMID: # 28583467  Hu, J. et al. 2017. Int. J. Biochem. Cell Biol. 89: 42-56.

PMID: # 26598923  Cui, XY. et al. 2016. Journal of thrombosis and haemostasis : JTH. 14: 387-96.

PMID: # 26926996  2016. J. Exp. Med. 213: 337-54.

PMID: # 25975820  Cursons, J. et al. 2015. Cell communication and signaling : CCS. 13: 26.

Citations 1 to 10 of 14 total

I want to know the solubility of the compound sc-205346A. can it be dissolved in Cell Growth medias, like DMEM, DEM-F12 etc.

Asked by: Rais Ansari
Thank you for your question. We have found that Hypoxia inducible factor-1α Inhibitor (CAS 934593-90-5) is insoluble in PBS, pH 7.4, so it is not likely to be soluble in cell growth media such as DMEM or DEM-F12.
Answered by: Technical Support
Date published: 2018-11-19

Can this antagonist be dissolved in Phosphate saline buffer?

Asked by: Kristeen
Thank you for your question. We have found this compound, Hypoxia inducible factor-1α Inhibitor (CAS 934593-90-5), to be insoluble in PBS, pH 7.2.
Answered by: Technical Support
Date published: 2019-02-25
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Rated 5 out of 5 by from Lai Lai, KG. et al. (PubMed 26135626) used the Hypoxia inducible factor-1 inhibitor to demonstrate that paclitaxel pretreatment is an effective radiosensitizing procedure against Hypoxia inducible factor-1 -expressing hepatoma and HLAC cells. -SCBT Publication Review
Date published: 2015-04-10
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