Transportan 

Transportan is an amphipathic cell-penetrating peptide containing 12 functional amino acids from the amino terminus of the neuropeptide galanin and mastoparan in the carboxyl terminus, connected via a lysine. Transportan interacts with galanin receptors and G-proteins, modulates GTPase activity, enters cells via direct translocation and endocytic pathways, accumulates in cytoplasmic, nuclear, and membranous structures, and delivers cargo including peptides, PNAs, proteins, siRNA, and liposomes^{[1][2][3][4][5][6][7][8][9][10][11][12]}.

Transportan (10 μM; 30 min/60 h) efficiently penetrates human Bowes melanoma cells at both 0°C and 37°C with comparable high uptake, distributes across the cytoplasm and nucleus, and has an internalization half-time of 3.4 min^[1].
Transportan (IC₅₀ 22 μM; 12 min at 30 °C) inhibits basal GTPase activity in Rin m5F cellular membranes with an IC₅₀ of 22 μM^[1].
Transportan inserts into phospholipid membranes at an oblique 65° angle relative to the surface, spans the bilayer with its mass center 1.7 Å into the first leaflet, and has a 32% α-helical structure in its central region^[1].
Transportan (1-10 μM; 1 min to 4 h) exhibits broad, cell-type-independent penetration, localizing to plasma membrane, cytosolic membranes, nuclear membrane, and nucleoli in Bowes’ melanoma cells and other mammalian cell lines, with temperature-dependent differences in intracellular distribution^[2].
Transportan binds to galanin receptors in Bowes’ melanoma cell membranes with a K_d value of 17.4 nM^[2].
Transportan (0.1 μM-0.1 mM; 12 min) inhibits basal GTPase activity in Bowes’ melanoma cell membranes with an EC₅₀ of 21.1 μM^[2].
Transportan (10 μM; 1 h) significantly increases bystander uptake of AgNPs, AuNPs, IONPs, and 70 kDa dextran in CHO-K1, H1975, and HeLa cells, as well as QD uptake in CHO-K1 and H1975 cells, and BSA uptake in CHO-K1 cells^[3].
Transportan (10 μM; 1-2 h) induces bystander nanoparticle uptake in CHO-K1 and HeLa cells via receptor-dependent macropinocytosis, with nanoparticles trafficking through early and late endosomes^[3].
Transportan (20 μM; 3 h) potently enhances liposome uptake in CHO, H1975, PC3, Neuro2A, Raw 264.7, and primary bone marrow-derived macrophages^[4].
Transportan (20 μM; 3 h) enables uptake of hydrophilic probe-loaded liposomes in CHO and H1975 cells^[4].
Transportan (20 μM; 3 h)-assisted liposome uptake in CHO cells is mediated primarily by macropinocytosis, with minor contributions from other endocytic pathways^[4].
Transportan (10 μM; 60 min at 37 °C) internalizes into human colon cancer Caco-2 cells, localizing to the nuclear membrane, nucleus, and cytoplasm, in an endocytosis-independent manner^[5].
Transportan (10 μM; 60 min at 37 °C) induces marked reorganization of actin filaments in confluent human colon cancer Caco-2 cells, producing thicker, more pronounced vertical stress fibres^[5].
Transportan (different concentrations; 48 h) co-administration significantly enhances the transfection efficiency of GFP-expressing lentivirus and AAV vectors in PC3 cells, Raw264.7 macrophage cell line, bone marrow-derived macrophages, and retinal pigment epithelium cells when incubated for 48 h, with limited cytotoxicity.
Transportan (TP) (2 μM; 12-48 h) efficiently delivers SASH1 siRNA to HT29 and HCT116 colorectal cancer cells, resulting in significant downregulation of SASH1 mRNA levels.
Fluorescently labeled transportan (0-30 μM; 1 h) shows concentration dependent and nonsaturable cellular uptake in triticale cv AC Alta mesophyll protoplasts, with increased relative fluorescence uptake observed at 5, 10, 20, and 30 μM after 1 h incubation at room temperature^[7].
Transportan (320 nmol; 30 h total) delivers functional siNP to inhibit PR8 H1N1 influenza virus replication in MDCK and A549 cells^[8].
Transportan (1 μM; 1 h) penetrates the membrane of HeLa human cervical cancer cells but does not enter HEL299 human non-cancer lung fibroblast cells^[9].

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

Transportan (20 μL of 2 mM; i.t.; single dose) significantly enhances the in vivo uptake of systemically administered liposomes in 4T1 breast tumors, increasing liposome-positive cells by over 5-fold^[4].
Transportan (800 nmol; i.v.; single dose) delivers functional siNP to inhibit influenza A virus replication in mice, with 100% survival observed in mice treated with the 50 nmol siNP dose complexed with Transportan^[8].
Transportan, as part of a PNA-transportan conjugate targeted to galanin receptor mRNA, regulates galanin receptor levels and modifies pain transmission in rats^[11].
Transportan (35-560 µg/kg; i.v.; single bolus injections; 15-minute intervals between escalating doses) induces a dose-dependent reduction in rat systemic blood pressure, with a maximal 35% decrease in mean arterial pressure observed at a dose of 280 µg/kg^[12].

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

2840.45

C₁₃₄H₂₂₇N₃₅O₃₂

203716-10-3

Solid

White to off-white

Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Lys-Ile-Asn-Leu-Lys-Ala-Leu-Ala-Ala-Leu-Ala-Lys-Lys-Ile-Leu-NH2

GWTLNSAGYLLGKINLKALAALAKKIL-NH2

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

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

* 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Soomets U, et al. Deletion analogues of transportan. Biochim Biophys Acta. 2000;1467(1):165-176.

  [2]. Pooga M, et al. Cell penetration by transportan. FASEB J. 1998;12(1):67-77.  [Content Brief]

  [3]. Li YX, et al. Transportan Peptide Stimulates the Nanomaterial Internalization into Mammalian Cells in the Bystander Manner through Macropinocytosis. Pharmaceutics. 2021;13(4):552. Published 2021 Apr 14.

  [4]. Li YX, et al. Co-administration of Transportan Peptide Enhances the Cellular Entry of Liposomes in the Bystander Manner Both In Vitro and In Vivo. Mol Pharm. 2022;19(11):4123-4134.

  [5]. Lindgren ME, et al. Passage of cell-penetrating peptides across a human epithelial cell layer in vitro. Biochem J. 2004;377(Pt 1):69-76.

  [6]. Pepe D, et al. Transportan in nanocarriers improves skin localization and antitumor activity of paclitaxel. Int J Nanomedicine. 2016;11:2009-2019. Published 2016 May 11.

  [7]. Chugh A, et al. Cellular uptake of cell-penetrating peptides pVEC and transportan in plants. J Pept Sci. 2008;14(4):477-481.

  [8]. Zhang C, et al. Transportan-derived cell-penetrating peptide delivers siRNA to inhibit replication of influenza virus in vivo. Drug Des Devel Ther. 2019;13:1059-1068. Published 2019 Apr 4.

  [9]. Izabela R, et al. Transportan 10 improves the anticancer activity of cisplatin. Naunyn Schmiedebergs Arch Pharmacol. 2016;389(5):485-497.

  [10]. Pooga M, et al. Cell penetrating PNA constructs regulate galanin receptor levels and modify pain transmission in vivo. Nat Biotechnol. 1998;16(9):857-861.

  [11]. Kaushik N, et al. Anti-TAR polyamide nucleotide analog conjugated with a membrane-permeating peptide inhibits human immunodeficiency virus type 1 production. J Virol. 2002;76(8):3881-3891.

  [12]. Basheer M, et al. Blood pressure modulation following activation of mast cells by cationic cell penetrating peptides. Peptides. 2011;32(12):2444-2451.