localization

FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors.

CCG-100602 inhibits RhoA/C-mediated, SRF-driven luciferase expression in PC-3 prostate cancer cells (IC50 :9.8 μM).

INI-43, an inhibitor of Nuclear Import-43, shows a significant cytotoxic effect on various cervical and oesophageal cancer cell lines by targeting Kpnβ1 and interferes with the nuclear localization of Kpnβ1 and known Kpnβ1 cargoes, NFAT, NFκB, AP-1 and NF

APX2039 is an orally active fungal Gwt1 enzyme inhibitor and a prodrug of the novel Gwt2096 inhibitor APX1.APX2039 exhibits potent anti-Kryptococcal activity against C. neoformans and C. gattii.APX2039 exhibits potent antifungal activity and blocks the localization of GPI (glycosylphosphatidylinositol) anchored cell wall mannoproteins. APX2039 has potent antifungal activity and blocks the localization of GPI (glycosylphosphatidylinositol)-anchored cell wall mannoproteins.APX2039 can be used to study cryptococcal meningitis (CM).

(-)-Epicatechin (Epicatechin) is an inhibitor of cyclooxygenase-1 (COX-1), inhibiting the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.

Lipase, triacylglycerol (Alkaline lipase) is a specific enzyme that plays an important role in the catabolism of triacylglycerol to glycerol and fatty acids and is required for the transfer of fatty acids to various tissues of the body, and whose transcriptional receipt of transcripts is subjected to nutrient/hormonal regulation and is capable of being upregulated by PPARγ,TNFα downregulation, and insulin-mediated downregulation of FOXO1 nuclear localization.

Methylene Violet 3RAX is a cationic dye, a potential photosensitizer in photodynamic therapy, with antitumor activity that alters the molecular structure of DNA, disrupts the modules of DNA, and induces the production of reactive monoclinic oxygen species, which are used to stain the mitochondria of cells.Methylene Violet 3RAX inhibits the subcellular localization of cancer cells by severing the Methylene Violet 3RAX inhibits subcellular localization of cancer cells, leading to cell death by cutting DNA strands in tumor cells.

Lemuteporfin is a light-activated photosensitizing agent that is rapidly internalized by viable cells, localizing within the cytoplasm and associating with mitochondria. This localization is a key characteristic that confers strong cytotoxic potential upon light activation. Lemuteporfin has demonstrated the ability to reduce sebaceous gland volume in preclinical animal studies. It is currently under investigation in relation to benign prostatic hyperplasia and in topical form for the management of androgenetic alopecia.

Rhodblock 6 is a Rho kinase (ROCK) inhibitor that specifically inhibits Rho kinase activity and the localization of phosphorylated MRLC (Myosin Regulatory Light Chain).

Nur77 modulator 1 is an effective Nur77 binder (KD = 3.58 μM) that up-regulates Nur77 expression, mediates its sub-cellular localization, induces Nur77-dependent ER stress and autophagy, and leads to cell apoptosis, demonstrating anti-hepatoma activity.

FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.

Ouabain octahydrate (Acocantherine) is a cardiac glycoside that inhibits Na(+)/K(+) ATPase. Ouabain octahydrate regulates transcription of MDR (increase, Pgp) and MRP (increase MRP1 and decrease CFTR, cyctic fibrosis transport receptor or cAMP-activated Cl- channel) genes, also alters localization of MRP1.

Stauprimide is a non-broad spectrum inhibitor that binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, which causes down-regulation of MYC transcription.

NHTD, a KRAS-PDEδ inhibitor, exerts its function by targeting the isoprenyl binding pocket of PDEδ, which alters the cellular localization of KRAS. This modification restricts the proliferation of cancer cells with KRAS mutations and induces cell apoptosis (Apoptosis). NHTD is utilized in the study of KRAS-driven non-small cell lung cancer (NSCLC).

PROTAC YAP degrader-1, a targeted proteolysis promoting chimeric molecule, both degrades the YAP protein and inhibits its nuclear localization. This compound is formulated with Demethyl-NSC682769 as the target protein ligand, and utilizes (R,S,R)-AHPC-PEG2-C2-boc, which is the E3 ubiquitin ligase ligand + Linker conjugate. The linker incorporated in the design is Acid-PEG2-C2-Boc.

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.

TRF2-IN-1 (compound F2) is a potent inhibitor of telomere repeat-binding factor 2 (TRF2). It exhibits antiproliferative activity and induces apoptosis. TRF2-IN-1 binds directly to the TRF2TRFH domain, selectively inhibiting TRF2 protein expression and telomere localization. Additionally, TRF2-IN-1 possesses anticancer properties and shows potential for osteosarcoma research.

SBI-0087702 enhances the cytoplasmic localization of ATF2 in melanoma cells. Induced translocation of ATF2 by SBI-0087702 to the mitochondria results in the loss of mitochondrial membrane integrity, thereby increasing apoptosis. Additionally, SBI-0087702 inhibits the growth and motility of melanoma cells. It also suppresses the phosphorylation of ATF2 at the Thr52 site by PKCε.

6-Alkyne-F-araNAD is an irreversible CD38 inhibitor that aids in better visualization of intracellular CD38 localization when used alongside other fluorescent probes (such as SR101−F-araNMN).

Rhodblock 1a is an inhibitor of the Rho kinase signaling pathway, which disrupts the localization and function of proteins within the Rho pathway. This interference hinders the proper formation of the cleavage furrow during cell division, leading to some cells either failing to form the cleavage furrow or forming a ruptured furrow, resulting in binucleated cells. Rhodblock 1a can be utilized for investigating cell division mechanisms and holds potential for research into cardiovascular diseases and cancer.

RH1115 is a modulator of autophagolysosomes. It induces changes in the characteristics of LAMP1 vesicles and alters lysosomal localization.

(+)-JJ-450 is a non-competitive antagonist that targets the androgen receptor (AR), inhibiting nuclear localization and transcriptional activity of AR under androgen-deprived conditions. In LN95 cells, (+)-JJ-450 is less effective than (-)-JJ-450 at inhibiting prostate-specific antigen (PSA) expression, likely due to its targeting of the AR ligand-binding domain (LBD). The compound works by promoting degradation of unbound AR within the nucleus and reducing AR binding to androgen response elements (AREs), thus inhibiting the transcriptional activity of AR and its splicing variants like ARv7. Additionally, (+)-JJ-450 is applicable for research in castration-resistant prostate cancer (CRPC) that is resistant to Enzalutamide (MDV3100).

CW8001 is a covalent Exportin-1 (XPO1) inhibitor with an EC50 value of 1 nM for inhibiting T cell activation. It prevents the nuclear localization of NFAT transcription factors, thereby suppressing the expression of inflammatory cytokines like IL-2. CW8001 shows potential for research in T cell-driven immune diseases such as graft-versus-host disease (GVHD).

Acid Ceramidase-IN-3 is an inhibitor of acid ceramidase (aCDase). It shows a pIC50 of 8.5 in enzymatic assays and a pIC50 of 6.8 in A375 melanoma cell assays for aCDase enzyme activity inhibition. Acid Ceramidase-IN-3 promotes hepatic stellate cell (HSC) inactivation, measured by dose-dependent reduction of COL1A1 and ACTA2 levels. Additionally, it inhibits aCDase activity in HSCs, facilitating their inactivation and inhibiting YAP/TAZ nuclear localization. The compound enhances the expression of dynein/kinesin-related proteins (NDE1, NDEL1, KIF3B, KIF15) while reducing the expression of proteins related to various signaling pathways (SARM1, RGAP1, PDGF-D, PDGFR-B). Acid Ceramidase-IN-3 is valuable for fibrosis disease research.