SF-1670


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

Description

SF-1670 is a specific phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor. SF-1670 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 SF-1670, providing a therapeutic strategy for improving the efficacy of granulocyte transfusion.

Product information

CAS Number: 345630-40-2

Molecular Weight: 307.34

Formula: C19H17NO3

Synonym:

SF1670

SF-1670

SF 1670

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

Smiles: CC(C)(C)C(=O)NC1=CC2=C(C=C1)C1=CC=CC=C1C(=O)C2=O

InChiKey: VZQDDSYKVYARDW-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month...

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

SF-1670 is a specific PTEN inhibitor with prolonged intracellular retention in neutrophils. SF-1670 enhances PtdIns(3, 4, 5)P3 signaling in transplanted neutrophils. SF-1670 also elevates Akt phosphorylation in murine cells. Consistent with the enhanced Akt phosphorylation, pretreatment with SF-1670 also significantly augments PtdIns(3, 4, 5)P3 level in mouse neutrophils. SF-1670-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, SF-1670 (500 nM)–pretreated neutrophils show nearly 70% higher (maximal) superoxide production than untreated neutrophils. HCT116 cells are pre-treated with the PTEN inhibitor SF-1670 (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). SF-1670 binds to the PTEN active site, resulting in elevated phosphatidylinositol (3, 4, 5) triphosphate signaling.

In Vivo:

SF-1670 (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.
  2. 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.
  3. 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.
  4. 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.
  5. 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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