SF-1670


Catalog No. size PriceQuantity
M6494-2 2mg solid $116
M6494-10 10mg solid $488

Description

Cas:345630-40-2

Product Information:

SF-1670 is a specific phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor. SF1670 specifically binds to the active site of PTEN inhibiting its activity with an IC50 value of 2 μM. The innate immune responses can be enhanced and the severity of neutropenia-related infection can be alleviated by augmenting phosphatidylinositol (3,4,5)-trisphosphate in transfused neutrophils with PTEN inhibitor SF1670, providing a therapeutic strategy for improving the efficacy of granulocyte transfusion.

 

Chemical Formula: C19H17NO3

 

Exact Mass: 307.1208

 

Molecular Weight: 307.349

 

Elemental Analysis: C, 74.25; H, 5.58; N, 4.56; O, 15.62

 

Synonym:

 

SF1670

SF-1670

SF 1670

 

Chemical Name:

N-(9,10-dihydro-9,10-dioxo-2-phenanthrenyl)-2,2-dimethyl-propanamide

 

InChi Key:

VZQDDSYKVYARDW-UHFFFAOYSA-N

 

InChi Code:

InChI=1S/C19H17NO3/c1-19(2,3)18(23)20-11-8-9-13-12-6-4-5-7-14(12)16(21)17(22)15(13)10-11/h4-10H,1-3H3,(H,20,23)

 

Smiles Code:

CC(C)(C)C(NC(C=C1C2=O)=CC=C1C3=C(C2=O)C=CC=C3)=O

 

 

Technical Data:

 

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

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

 

In Vitro:

SF1670 is a specific PTEN inhibitor with prolonged intracellular retention in neutrophils. SF1670 enhances PtdIns(3,4,5)P3 signaling in transplanted neutrophils. SF1670 also elevates Akt phosphorylation in murine cells. Consistent with the enhanced Akt phosphorylation, pretreatment with SF1670 also significantly augments PtdIns(3,4,5)P3 level in mouse neutrophils. SF1670-induced Akt hyperactivation is abolished in PTEN-null neutrophils, further demonstrating that this effect is mediated by specific inhibition of PTEN activity. At 500 nM fMLP stimulation, SF1670 (500 nM)–pretreated neutrophils show nearly 70% higher (maximal) superoxide production than untreated neutrophils. HCT116 cells are pre-treated with the PTEN inhibitor SF1670 (2 μM) for 24 h (untreated HCT116 cells served as control); treated cells are subsequently plated under non-adherent conditions with added MET (60 μM), Lun (2 μM), or Gen (2 μM). SF1670 binds to the PTEN active site, resulting in elevated phosphatidylinositol (3,4,5) triphosphate signaling.

 

In Vivo:

SF1670 (3 mg/kg; i.p.) triggers postconditioning after inducing cerebral global ischaemia (17 min) and reperfusion (24 h)‐induced injury via occlusion of both carotid arteries in mice.

 

 

References

 

  1. Chen JH, Lee MS, Wang CP, Hsu CC, Lin HH. Autophagic effects of Hibiscus sabdariffa leaf polyphenols and epicatechin gallate (ECG) against oxidized LDL-induced injury of human endothelial cells. Eur J Nutr. 2016 Jun 18. [Epub ahead of print] PubMed PMID: 27318926.

 

  1. Zhou X, Zang X, Ponnusamy M, Masucci MV, Tolbert E, Gong R, Zhao TC, Liu N, Bayliss G, Dworkin LD, Zhuang S. Enhancer of Zeste Homolog 2 Inhibition Attenuates Renal Fibrosis by Maintaining Smad7 and Phosphatase and Tensin Homolog Expression. J Am Soc Nephrol. 2016 Jul;27(7):2092-108. doi: 10.1681/ASN.2015040457. PubMed PMID: 26701983; PubMed Central PMCID: PMC4926973.

 

  1. Montales MT, Simmen RC, Ferreira ES, Neves VA, Simmen FA. Metformin and soybean-derived bioactive molecules attenuate the expansion of stem cell-like epithelial subpopulation and confer apoptotic sensitivity in human colon cancer cells. Genes Nutr. 2015 Nov;10(6):49. doi: 10.1007/s12263-015-0499-6. PubMed PMID: 26506839; PubMed Central PMCID: PMC4623856.

 

  1. Lin HH. In Vitro and in Vivo Atheroprotective Effects of Gossypetin against Endothelial Cell Injury by Induction of Autophagy. Chem Res Toxicol. 2015 Feb 16;28(2):202-15. PubMed PMID: 25622137.

 

  1. Spinelli L, Lindsay YE, Leslie NR. PTEN inhibitors: an evaluation of current compounds. Adv Biol Regul. 2015 Jan;57:102-11. doi: 10.1016/j.jbior.2014.09.012. PubMed PMID: 25446882.

 

Products are for research use only. Not for human use.

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