Surfen dihydrochloride  (Synonyms: Aminoquinuride dihydrochloride)

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

Surfen (3 μM) dihydrochloride binds to glycosaminoglycans (GAGs)^[1].
Surfen (1 mg) dihydrochloride neutralizes the anticoagulant activity of both unfractionated and low molecular weight heparins^[1].
Surfen dihydrochloride inhibits the activity of recombinant uronyl 2-O-sulfotransferase, with an IC₅₀ of ~2 μM^[1].
Surfen (1-≥5 μM) dihydrochloride inhibits cell attachment in a dose-dependent manner, and completely inhibits HSV-1 infection in CHO cells^[1].
Surfen (5 μM) dihydrochloride effectively inhibits neural differentiation and promotes the maintenance of pluripotency in mouse embryonic stem cells (mESCs)^[2].
Surfen (2.5-20 μM) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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) dihydrochloride delays remyelination of the lesions in the Lysolecithin (LPC)-induced demyelination mouse model^[5].
Surfen (20 mg/kg; i.p.; daily; 3 consecutive days) dihydrochloride 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.

445.34

C₂₁H₂₂Cl₂N₆O

5424-37-3

Solid

Off-white to gray

O=C(NC1=CC=C2N=C(C)C=C(N)C2=C1)NC3=CC=C4N=C(C)C=C(N)C4=C3.Cl.Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [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]