trafficking

Elexacaftor (VX-445) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. It promotes the processing and trafficking of CFTR, increases the amount of CFTR on the cell surface, and improves the processing and trafficking of Phe508del CFTR protein.

UNC10217938A HCl (UNC7938 HCl) is a 3-deazapteridine analog. UNC10217938A HCl exhibits strong oligonucleotide enhancing effects. UNC10217938A HCl can modulate their intracellular trafficking and release from endosomes, leading to enhance oligonucleotides effects. UNC10217938A HCl also enhances the effects of siRNA and antisense oligonucleotides.

LKM38, a novel diazolidinyl cholesterol probe, is a promising cholesterol mimetic.LKM38 both maintains cholesterol-resistant cell growth and appropriately regulates key cholesterol homeostatic pathways.LKM38 can be a powerful tool for studying cholesterol protein interactions and trafficking.

Lumacaftor (VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein. It enhances F508del-CFTR protein maturation in FRT cells (EC50: 100 nM).

Endosidin 7, a specific inhibitor of callose synthase, organizes callose deposition during plant cytoplasmic division without affecting endosomal transport during interphase or cytoskeletal organization, preventing late cytokinesis.

(E)-KPT330 is a CRM1-selective inhibitor of nuclear export. It inhibits protein trafficking from the nucleus and induces cell cycle arrest and apoptosis in mesothelioma cells.

PD 128042 (CI 976) is a potent, orally active, and selective ACAT inhibitor (IC50: 73 nM) as well as a lysophospholipid acyltransferase (LPAT) inhibitor. CI 976 inhibits Golgi-associated LPAT activity (IC50: 15 μM) and multiple membrane trafficking steps.

Navarixin (MK-7123)(SCH527123) is a novel, selective CXC chemokine receptor 2(CXCR2) antagonist that inhibits neutrophil activation and modulates neutrophil trafficking in animal models, characteristics that may be beneficial in the treatment of conditions with unbalanced pulmonary neutrophilia.

Ceapin-A7, with an IC50 of 0.59 μM, selectively inhibits ATF6α signaling in response to ER stress. This compound is instrumental in investigating ATF6α's activation mechanism and its function in pathological conditions.

Retro-2 (2-{[(5-methyl-2-thienyl)methylene]amino}) is a plant toxin ricin inhibitor, itprotects HeLa cells against Ricin, Stx1 and Stx2, selectively blocks retrograde toxin trafficking at the early endosome-TGN (trans-Golgi network) interface.

CCR4 antagonist 2 (Compound 31) is a novel, potent, orally bioavailable small molecule antagonist of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+ flux and [chemotaxis] CTX at 40 nM and 70 nM, respectively.

G0507 is a pyrrolopyrimidinedione compound that serves as a potent inhibitor of Escherichia coli growth, effectively inducing the extracytoplasmic σE stress response. It acts as a valuable chemical probe, specifically designed to dissect lipoprotein trafficking in Gram-negative bacteria. Notably, G0507 demonstrates strong inhibitory activity against the LolCDE ABC Transporter.

Retro-2 cycl is a dihydroquinazolinone (DHQZ) retrograde trafficking inhibitor. Retro-2 cycl (RN 1-001) inhibits JCPyV and HPV16 pseudovirus(IC50s of 54 μM and 160 μM, respectively),with antiviral agent.

DHQZ 36 is a potent retrograde trafficking inhibitor. It has potent anti-parasite activity. DHQZ 36 inhibits Leishmania amazonensis infection in macrophages (EC50: 13.63 μM).

TRV045 is a selective agonist of the sphingosine-1-phosphate (S1P) subtype 1 receptor and does not impact lymphocyte trafficking. It possesses antiepileptic properties.

biotinylated anandamide analog acts as a probe for visualizing the accumulation and intracellular trafficking of anandamide

CESTRIN is a cellulose synthase trafficking probe that acts by inhibiting cellulose deposition and interferes with the trafficking of cellulose synthase complexes and their associated proteins KORRIGAN1 and POM2/CSI1.

D011-2120 is an agent of antiviral that acts by blocking microtubule polymerization, disrupting the Golgi complex and inhibiting viral trafficking to the plasma membrane during virus egress.

EGA inhibits the intoxication of lethal toxins and prevents the entry of a variety of other acid-dependent bacterial toxins and viruses into mammalian cells.EGA is a powerful tool for the study of membrane trafficking and can be used to treat infectious diseases.

Okicenone is an antibiotic, interferring with HuR RNA binding, HuR trafficking, T-cell activation and cytokine expression.

PPQ-581 is an anti-influenza agent. PPQ-581 interrupts the crucial RNP trafficking, resulting in influenza replication inhibition, preventing virus-induced cytopathic effects.

SPM-242 is an orthosteric agonist of Sphingosine 1-phosphate (S1P) and a bitopic antagonist. S1P is a lysophospholipid signaling molecule that regulates important biological functions, including vascular development and lymphocyte trafficking, by activat

KM11060 is a novel corrector of the F508del-CFTR trafficking defect, Correcting F508del-CFTR trafficking, increasing the amount of functional CFTR at the plasma membrane.

PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3/Akt PH domain binding, that is designed for more favorable solubility in vivo. 3,5-dimethyl PIT-1 inhibits PI3K/Akt signaling (IC50 = 27 μM), suppressing PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 36 μM). 4T1 breast cancer growth is significantly attenuated in BALB/c mice with a dose of 1 mg/kg of 3,5-dimethyl PIT-1 per day.