Surfen  (Synonyms: Aminoquinuride)

Surfen is a potent heparan sulfate antagonist. Surfen inhibits FGF2 binding and signal transduction. Surfen binds to glycosaminoglycans and reduces tau hyperphosphorylation. Surfen inhibits the activity of recombinant uronyl 2-O-sulfotransferase with an IC₅₀ of approximately 2 μM. Surfen inhibits HSV-1 viral infection. Surfen inhibits neural differentiation, delays remyelination, and alleviates EAE^{[1][2][3][4][5][6]}.

Surfen (3 μM) binds to glycosaminoglycans (GAGs)^[1].
Surfen (1 mg) neutralizes the anticoagulant activity of both unfractionated and low molecular weight heparins^[1].
Surfen inhibits the activity of recombinant uronyl 2-O-sulfotransferase, with an IC₅₀ of ~2 μM^[1].
Surfen (1-≥5 μM) inhibits cell attachment in a dose-dependent manner, and completely inhibits HSV-1 infection in CHO cells^[1].
Surfen (5 μM) effectively inhibits neural differentiation and promotes the maintenance of pluripotency in mouse embryonic stem cells (mESCs)^[2].
Surfen (2.5-20 μM) reduces the proliferation of murine T cells activated with anti-CD3/CD28 antibody-coated T cell expander beads^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Surfen (3 μM; 2 days) significantly reduces tau hyperphosphorylation, rescues spinal motoneuron axon-branching defects and behavioral deficits in Tg[HuC::hTau^P301L; DsRed] embryos of zebrafish tauopathy model^[4].
Surfen (5 mg/kg; i.p.; every other day) alleviates clinical symptoms and reduces the infiltration of CD4 positive T cells and macrophages into the central nervous system in the experimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis in mice^[5].
Surfen (100 μM; injection into the right burr hole) delays remyelination of the lesions in the Lysolecithin (LPC)-induced demyelination mouse model^[5].
Surfen (20 mg/kg; i.p.; daily; 3 consecutive days) inhibits the proliferation of T cells activated by anti-CD3 antibody in mice^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

372.42

C₂₁H₂₀N₆O

3811-56-1

O=C(NC1=CC2=C(N=C(C)C=C2N)C=C1)NC3=CC4=C(N=C(C)C=C4N)C=C3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Schuksz M, et al. Surfen, a small molecule antagonist of heparan sulfate. Proc Natl Acad Sci U S A. 2008 Sep 2;105(35):13075-80.  [Content Brief]

  [2]. Huang ML, et al. Small Molecule Antagonist of Cell Surface Glycosaminoglycans Restricts Mouse Embryonic Stem Cells in a Pluripotent State. Stem Cells. 2018 Jan;36(1):45-54.  [Content Brief]

  [3]. Varatharajan A, et al. Visual determination of heparin in serum utilizing surfen-induced aggregation emission enhancement of gold nanoclusters and heparin-induced fluorescence enhancement of surfen. Spectrochim Acta A Mol Biomol Spectrosc. 2025 Apr 15;339:126251.  [Content Brief]

  [4]. Alavi Naini SM, et al. Surfen and oxalyl surfen decrease tau hyperphosphorylation and mitigate neuron deficits in vivo in a zebrafish model of tauopathy. Transl Neurodegener. 2018 Mar 16;7:6.  [Content Brief]

  [5]. Warford JR, et al. Surfen, a proteoglycan binding agent, reduces inflammation but inhibits remyelination in murine models of Multiple Sclerosis. Acta Neuropathol Commun. 2018 Jan 4;6(1):4.  [Content Brief]

  [6]. Warford J, et al. Murine T cell activation is regulated by surfen (bis-2-methyl-4-amino-quinolyl-6-carbamide). Biochem Biophys Res Commun. 2014 Jan 10;443(2):524-30.  [Content Brief]