Low molecular weight protamine  (Synonyms: LMWP; TDSP5)

Low molecular weight protamine (LMWP;TDSP5) is a truncated arginine-rich protamine peptide, as well as a heparin/low-molecular-weight heparin antidote and a cell-penetrating delivery carrier. Low molecular weight protamine neutralizes heparin-induced anticoagulant activities, including aPTT, anti-Xa and anti-IIa activities, and also neutralizes anti-Xa activity of commercially available low-molecular-weight heparin preparations. Low molecular weight protamine translocates across mammalian cell membranes, delivers conjugated impermeable molecules across tumor tissues, enhances skin permeability of conjugated epidermal growth factor, and accelerates wound healing when conjugated with epidermal growth factor. Low molecular weight protamine retains the in vitro cell proliferation activity of conjugated EGF, and also enables site-specific conjugation with peptides or proteins via genetic recombination. Low molecular weight protamine can be used in studies related to colon adenocarcinoma, skin wounds and diabetic skin wounds^[1][2][3].

Low molecular weight protamine (18 μg/U; 3 minutes) completely neutralizes the aPTT-clotting activity of 5 U/mL heparin in human plasma at a TDSP₅/heparin ratio of 18 μg/U^[1].
Low molecular weight protamine (12 μg/U; 2 minutes, 10 minutes) completely neutralizes the anti-IIa activity of 0.5 U/mL heparin in human plasma at a TDSP₅/heparin ratio of 12 μg/U^[1].
Low molecular weight protamine (4.5 mg/mL, 22 μg/U; 60 minutes) alone (4.5 mg/mL) causes only 30% complement consumption in human serum, and TDSP5-heparin complexes (22 μg/U ratio, with 2.5-10 U/mL heparin) cause ~50% complement consumption, showing significantly reduced complement activation potential compared to protamine^[1].
Low molecular weight protamine (63 μM; 2 hours) exhibits significantly reduced cross-reactivity with mouse antiprotamine antibodies, requiring a concentration of 63 μM to achieve 50% inhibition of antibody binding in a competitive ELISA^[1].
LMWP-gelonin conjugate inhibits protein synthesis in a cell-free rabbit reticulocyte lysate system with an IC₅₀ of 23 pM^[2].
FITC-labeled LMWP (TDSP5) (0.2 μM; 30 min) is taken up by 293T, HeLa, CT-26, MCF-7, NIH3T3, and MG63 cells with high efficiency, equivalent to TAT peptide, and this uptake is unaffected by 10% serum^[2].
Low molecular weight protamine (0.2 μM; 30 min) localizes to the cytoplasm of HeLa cells, delivers covalently conjugated gelonin to the cytoplasm of CT-26 cells, and delivers covalently conjugated phalloidin to the cytoplasm of MG63 cells to label cytoskeletons without permeabilization^[2].
Low molecular weight protamine (0.01-10.0 mM; 72 h) exhibits minimal cytotoxicity to 293T cells, with less than 10% reduction in cell viability at concentrations up to 10.0 mM after 72 h of incubation^[2].
LMWP-gelonin conjugate (48 h) exhibits potent dose-dependent cytotoxicity against CT-26 colon adenocarcinoma cells with an IC₅₀ of 39 pM after 48 h of incubation^[2].

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

Low molecular weight protamine-gelonin conjugate (110 µg; peritumoral injection; nine times over 15 days) achieves nearly complete tumor regression in CT-26 tumor-bearing BALB/c mice, with an average final tumor mass of 0.33 g^[2].

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

1880.18

C₇₂H₁₄₂N₄₄O₁₆

121052-30-0

Solid

White to off-white

Val-Ser-Arg-Arg-Arg-Arg-Arg-Arg-Gly-Gly-Arg-Arg-Arg-Arg

VSRRRRRRGGRRRR

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.

* 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]. Chang LC, et al. Low molecular weight protamine (LMWP) as nontoxic heparin/low molecular weight heparin antidote (II): in vitro evaluation of efficacy and toxicity. AAPS PharmSci. 2001;3(3):E18.  [Content Brief]

  [2]. Park YJ, et al. Nontoxic membrane translocation peptide from protamine, low molecular weight protamine (LMWP), for enhanced intracellular protein delivery: in vitro and in vivo study. FASEB J. 2005;19(11):1555-1557.  [Content Brief]

  [3]. Choi JK, et al. The effect of epidermal growth factor (EGF) conjugated with low-molecular-weight protamine (LMWP) on wound healing of the skin. Biomaterials. 2012;33(33):8579-8590.  [Content Brief]