PTX

Pentoxifylline (PTX) modulates immunologic activity by stimulating cytokine production. Pentoxifylline is a methylxanthine derivative that inhibits phosphodiesterase and affects blood rheology. It also inhibits platelet aggregation and improves blood flow by increasing erythrocyte and leukocyte flexibility.

IR820-PTX is a nanoparticle composed of IR-820 and paclitaxel that is highly permeable and tumor-targeting.IR820-PTX can be used for near-infrared fluorescence imaging and tumor diagnostics.9-cis-Retinoic Acetylcholine (RAC) is a nanoparticle that is highly permeable and tumor-targeting.

PTX80 is an antagonist of p62, with an IC50 value of 31.18 nM. It has been shown to reduce tumor volume in a HCT116 colorectal cancer mouse xenograft model.

AMPTX-1 is a molecular glue functioning as a potent, selective, and reversible covalent degrader of BRD9 by recruiting it to the E3 ligase DCAF16.

GpTx-1 exhibits potent selectivity as a NaV1.7 antagonist, demonstrating an inhibition concentration (IC50) of 10 nM [1].

GpTx-1 TFA is a polypeptide NaV1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. It exhibits potent inhibitory activity on the NaV1.7 channel with an IC50 value of 10 nM, demonstrating excellent selectivity over NaV1.4 (IC50 = 0.301 μM) and NaV1.5 (IC50 = 4.20 μM) with >20-fold and >950-fold selectivity, respectively.

Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.

Triciribine phosphate (VD 002) is a highly selective AKT inhibitor that induces cell cycle arrest and cysteinyl asparagin-dependent apoptosis, inhibits neovascularization, and can be used in the study of leukemia.

OTX008 (PTX008) is a selective galectin-1 inhibitor.

ABCB1-IN-2 (compound 16q) is a functional inhibitor that directly binds and stabilizes the ABCB1 protein structure without altering its expression and subcellular localization. This compound enhances the sensitivity of MCF-7 ADR cells to paclitaxel (PTX) by increasing PTX accumulation and inhibiting the ABCB1-mediated accumulation and excretion of luciferin Rh123. As a potent ABCB1-mediated multidrug resistance (MDR) reversal agent, ABCB1-IN-2 effectively reverses MDR.

ABCB1-IN-3 (Compound K27) is an orally active ABCB1 inhibitor that induces apoptosis. It binds directly to ABCB1, inhibiting its efflux function and maintaining stable intracellular paclitaxel (PTX) concentrations without affecting the normal expression of ABCB1. In vitro, ABCB1-IN-3 significantly increases ABCB1-mediated multidrug resistance (MDR) sensitivity to PTX, leading to cell cycle arrest and inhibition of cell proliferation. When combined with PTX, ABCB1-IN-3 demonstrates strong antitumor effects in vivo without causing toxicity.

PhTX-343, also known as Philanthotoxin 343, is synthetic analogue of Philanthotoxin 433. PhTX-343 blocks NMDA-gated ion channels; synthetic analog of the wasp polyamine amide toxin δ-philanthotoxin.

6α-hydroxy Paclitaxel (6α-OH-PTX) is a major metabolite of the anticancer compound paclitaxel and is partially cytotoxic.

The acyl amides are a family of endogenous lipids that act as potent modulators of pain and inflammation. The best characterized members of this family are the arachidonoyl amides, which includes N-arachidonoyl ethanolamide (AEA; anandamide). N-palmitoyl glycine (PalGly) contains an 18-carbon saturated fatty acid that is amide-linked to glycine and is structurally similar to the phospholipid-derived N-acyl ethanolamines. Endogenously produced in rat skin and spinal cord, PalGly is present in 100-fold greater amounts in skin and 3-fold greater in brain compared to AEA. Injection of 0.43 μg PalGly in rat hindpaw inhibits heat-induced firing of nociceptive neurons in rat dorsal horn. PalGly treatment induces transient calcium influx in native dorsal root ganglion (DRG) cells and in the PTX-sensitive, DRG-like cell line F-11 (EC50 = 5.5 μM).

P-gp BCRP-IN-1 (compound 19) is a relatively safe, orally active, and efficient inhibitor of the efflux transporters P-gp and BCRP, which reverses resistance and enhances the oral bioavailability of Paclitaxel (PTX) [1].

WS-898 is a potent inhibitor of ABCB1 that reverses resistance to paclitaxel (PTX) in drug-resistant SW620 Ad300, KB-C2 and HEK293 ABCB1 cells with IC50 values of 5.0, 3.67 and 3.68 nM, respectively.

Ki23057 is a a FGFR2 inhibitor, which enhances the chemosensitivity of drug-resistant gastric cancer cell lines when used in combination with chemotherapeutic drugs. Ki23057 might be therapeutically promising for treating drug-resistant gastric cancer cells, especially when used in combination with SN38, PTX, or VP16. The apoptosis process might be the main mechanism underlying the synergistic effect of these combinations. The ERCC1 and p53 genes may play an integral role in the synergism between Ki23057 and chemotherapeutic agents in drug-resistant cell lines. (source: Cancer Lett. 2011 Aug 1;307(1):47-52).

WS-691 is a highly Potent and Orally Active ABCB1 Modulator. WS-691 significantly increased sensitization of ABCB1-overexpressed SW620 Ad300 cells to paclitaxel (PTX) (IC50 = 22.02 nM). WS-691 significantly increased the intracellular concentration of PTX and [3H]-PTX while decreasing the efflux of [3H]- PTX in SW620 Ad300 cells by inhibiting the efflux function of ABCB1. WS-691 could stabilize ABCB1 by directly binding to ABCB1 WS-691 increased the sensitivity of SW620 Ad300 cells to PTX in vivo without observed toxicity.

NOD1 2 Antagonist-1 is a potent dual inhibitor of nucleotide-binding oligomerization domain-like receptors 1 and 2 (NOD1 2), displaying inhibitory concentrations (IC50) of 1.13 μM for NOD1 and 0.77 μM for NOD2. It exhibits an acceptable half-life (T1 2) of 67.6 minutes. Additionally, NOD1 2 Antagonist-1 enhances the antitumor efficiency of Paclitaxel (PTX).

LH2 peptide is a pH-responsive, cell-penetrating peptide dimer with the amino acid sequence LHHLCHLLHHLCHLAG. It increases uptake in tumor cells in slightly acidic environments (such as the tumor microenvironment) through histidine residue protonation (pKa approximately 6). When conjugated with the anticancer agent paclitaxel to form PTX-LH2, it demonstrates superior tumor inhibition compared to paclitaxel alone in a subcutaneous breast tumor model. LH2 peptide holds promise as a delivery vector for cancer research.