cellular uptake

JPH203 (KYT-0353) is a potent and specific inhibitor of L-type amino acid transporter protein 1 (LAT-1). JPH203 inhibits cellular uptake of leucine, inhibits cell proliferation, induces apoptosis, and possesses anti-inflammatory and anti-tumor activities.

OMDM-6 is a dual agonist of TRPV1(EC50 = 75 nM) and CB1 (Ki = 3.2 μM). OMDM-6 inhibits anandamide cellular uptake with a Ki of 7.0 μM.

Copper histidine inhibited Ctr1-mediated cellular uptake of oxaliplatin in vitro without altering oxaliplatin accumulation of platinum or neurotoxicity in DRG tissues in vivo. Copper histidine is administered orally for the treatment of Menkes disease.

hydrocotarnine is an inhibitor of Cbl.

OMDM-1 ((Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide) is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor with a Ki of 2.4 μM.

OMDM-2 is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor(Ki of 3.0 μM).

OMDM-3 is a selective and metabolically stable anandamide cellular uptake (ACU) inhibitor with a Ki of 16.6 μM.

OMDM-4 is a selective and metabolically stable anandamide cellular uptake (ACU) inhibitor with a Ki of 17.7 μM.

OMDM-5 is a selective anandamide cellular uptake (ACU)inhibitor(Ki of 4.8 μM).

BAMB-4 (ITPKA-IN-C14) is a highly membrane-permeable inhibitor of inositol-1,4,5-trisphosphate-3-kinase A (ITPKA), effectively suppressing the metastasis-promoting effect of ITPKA in lung tumor cells (with IC50 of 37 μM in ADP-Glo Assay).

MeIm (compound 7), a peptide mimetic targeting PCSK9, exhibits cholesterol-lowering properties by enhancing the cellular uptake of LDL (EC 50 = 6.04 μM) and obstructing PCSK9's interaction with LDLR (IC 50 = 11.2 μM). This compound is useful for research in cardiovascular diseases.

STAT3 HDAC-IN-2 (compound 18), a dual inhibitor of STAT3 and HDAC, promotes autophagy and apoptosis. This compound features an amphiphilic hydroxamic acid hybrid structure, derived from the natural product isopropanol lactone (IAL), and functions as a nanoscale anticancer agent. It has the ability to self-assemble into nanoparticles in aqueous environments, leading to enhanced tumor tissue accumulation, increased cellular uptake, and improved anticancer efficacy compared to its free state.

Boc-Pro-OMe (Boc-L-proline methyl ester) is a lipid compound utilized in liposome preparation. Liposomes consist of concentric phospholipid bilayer vesicles, which serve as vital components in constructing drug delivery systems for anticancer and anti-infection applications. These systems effectively encapsulate high-polarity water-soluble payloads within the internal aqueous space of the liposome, while lipophilic payloads are integrated into and become part of the lipid bilayer. This compound is particularly effective for delivering antisense oligonucleotides, addressing issues of low cellular uptake and rapid bodily excretion.

(2S)-3-Keto sphinganine (d6:0) ((2S)-3-Keto-C6-dihydrosphingosine) hydrochloride is a lipid compound utilized in the preparation of liposomes. Liposomes, characterized by concentric phospholipid bilayer vesicles, are critical in constructing drug delivery systems for anti-cancer and anti-infection applications. They effectively encapsulate hydrophilic solutes within their aqueous interiors and incorporate lipophilic cargoes into their phospholipid bilayers, making them integral to the bilayer structure. This compound is particularly valuable in delivering antisense oligonucleotides, addressing challenges such as inefficient cellular uptake and rapid loss in the body.

1-Stearoyl-2-docosahexaenoyl-sn-glycero-3-phosphoethanolamine (18:0-22:6 PE) is a lipid compound utilized in the preparation of liposomes. Liposomes, forming the central component of concentric phospholipid bilayer vesicles, are pivotal in constructing drug delivery systems for anti-cancer and anti-infection applications. They effectively encapsulate hydrophilic payloads within their aqueous internal spaces, while lipophilic compounds are integrated into and become part of the lipid bilayer. This compound is particularly effective for delivering antisense oligonucleotides, addressing challenges such as inefficient cellular uptake and rapid loss in the body.

NH2-GG-DSPE is a lipid compound utilized in liposome formulation. Liposomes, having concentric phospholipid bilayer vesicles, are crucial components in constructing drug delivery systems for anti-cancer and anti-infection applications. This compound enables the encapsulation of highly polar water-soluble cargoes within the internal aqueous spaces of liposomes, while lipophilic cargoes can integrate into and become part of the lipid bilayers. NH2-GG-DSPE is particularly effective for delivering antisense oligonucleotides, overcoming challenges such as inefficient cellular uptake and rapid loss in the body.

1,2-Dilinoleoyl-sn-glycero-3-phospho-L-serine sodium is a lipid compound utilized in the formulation of liposomes. Liposomes, composed of concentric phospholipid bilayer vesicles, serve as integral components in drug delivery systems aimed at oncology and anti-infection treatments. They efficiently encapsulate hydrophilic (highly polar) solutes within their aqueous interior, while lipophilic solutes are integrated into and become part of the lipid bilayer. This compound is particularly effective in delivering antisense oligonucleotides, addressing challenges such as poor cellular uptake and rapid degradation in the body.

LXQ-87 is an orally administered, non-competitive inhibitor of PTP1B with an IC50 of 1.061 μM, demonstrating hypoglycemic activity. It alleviates insulin resistance and enhances cellular glucose uptake, making it useful for type 2 diabetes research.

Antifolate C1 is an inhibitor of de novo purine biosynthesis. Antifolate C1 has selectivity for cellular uptake by high affinity folate receptors and the proton-coupled folate transporter (PCFT) over the reduced folate carrier (RFC).

Phenanthriplatin, also known as cis-[Pt(NH3)2-(phenanthridine)Cl]NO3, is a new drug candidate. It belongs to a family of platinum(II)-based agents which includes cisplatin, oxaliplatin and carboplatin. Phenanthriplatin Acts As a Covalent Poison of Topoiso

DSPE-PEG(2000)-amine is a PEGylated derivative of 1,2-distearoyl-sn-glycero-3-PE . It has been used in the synthesis of solid lipid and thermosensitive liposomal nanoparticles for the delivery of anticancer agents.1,2,3DSPE-PEG(2000)-amine has also been used in the synthesis of fluorescein isothiocyanate-loaded mesoporous silica nanoparticles for imaging applications.4It can be conjugated to a variety of functional molecules for improved cellular targeting and uptake of DSPE-PEG(2000)-amine-containing nanoparticles.4,5 1.Sloat, B.R., Sandoval, M.A., Li, D., et al.In vitro and in vivo anti-tumor activities of a gemcitabine derivative carried by nanoparticlesInt. J. Pharm.409(1-2)278-288(2011) 2.Abd-Rabou, A.A., Bharali, D.J., and Mousa, S.A.Taribavirin and 5-fluorouracil-loaded pegylated-lipid nanoparticle synthesis, p38 docking, and antiproliferative effects on MCF-7 breast cancerPharm. Res.35(4)76(2018) 3.Affram, K., Udofot, O., Singh, M., et al.Smart thermosensitive liposomes for effective solid tumor therapy and in vivo imagingPLoS One12(9):e0815116(2017) 4.Wang, L.-S., Wu, L.-C., Lu, S.-Y., et al.Biofunctionalized phospholipid-capped mesoporous silica nanoshuttles for targeted drug delivery: Improved water suspensibility and decreased nonspecific protein bindingACS Nano4(8)4371-4379(2010) 5.Wen, X., Wang, K., Zhao, Z., et al.Brain-targeted delivery of trans-activating transcriptor-conjugated magnetic PLGA/lipid nanoparticlesPLoS One9(9):e106652(2014)

4-hydroxy-3-Methoxyphenylglycol (piperazine salt) is a metabolite of norepinephrine derived in part by deamination of normetanephrine or by O-methylation of dihydroxyphenylglycol after cellular uptake of either intermediate. It is released into the blood and cerebrospinal fluid and has been used as a biochemical index of recent sympathetic nervous system activity.

MOPIPP is a novel indolebased chalcone that can cross the blood-brain barrier. MOPIPP inhibits the tumor progression agaisnt glioblastoma cells. MOPIPP induces cellular vacuolization as well as increases autophagosomes numbers. MOPIPP also triggers methuosis and distrupts glucose uptake and glycolytic metabolism [1] [2] [3].

Baicalein monohydrate is an inhibitor of 12-lipoxygenase, leukotriene biosynthesis and release of lysosomal enzymes. It also inhibits cellular Ca2+ uptake and mobilization and adjuvant-induced arthritis.