it 139

BOLD-100 free base (NKP-1339; IT-139), a ruthenium-based anticancer agent, inhibits stress-induced GRP78 upregulation, thus disrupting endoplasmic reticulum (ER) homeostasis. This action induces ER stress and unfolded protein response (UPR), interfering with the intricate relationship between ER-stress response, lysosome dynamics, and autophagy execution.

NKP-1339 (IT-139) induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway.

TD139 is a small molecule inhibitor of inhaled galectin-3 (Gal-3) with potential anti-fibrotic activity, commonly used in the study of idiopathic pulmonary fibrosis.

ELB-139 is a GABAA receptor agonist that can be used to study depression and epilepsy.

EGFR-IN-139 (compound PD 18) is an EGFR inhibitor with IC50 values of 12.88 nM (wild type), 10.84 nM (L858R/T790M), and 42.68 nM (L858R/T790M/C797S). It demonstrates significant anticancer activity against the A549 and H1975 cancer cell lines, which express high levels of EGFR. EGFR-IN-139 exhibits strong selectivity for cancer cells and can be utilized in research on non-small cell lung cancer (NSCLC).

Antitumor agent-139 (compound 9b) is a gold (I) complex targeting liver and mitochondria, capable of generating reactive oxygen species (ROS) and facilitating DNA excretion. It inhibits tumor growth in patient-derived liver cancer xenograft models.

Antifungalagent 139 (Compound li) is an antifungal agent that demonstrates antifungal activity against Colletotrichum gloeosporioides by inhibiting CgSfu1 and CgRidA. It completely inhibits the growth of hyphae, conidial germination, and appressorium formation, with an EC50 of 18 μg/mL. Antifungalagent 139 effectively blocks the infection of host plants, such as tulip trees and cedar, by the pathogen. This compound is valuable for studying anthracnose disease.

mmu-miR-139-3p Antagomir is modified with a high-affinity cholesterol group. This miRNA antagomir inhibits the function of mature miRNA by specifically binding to it, thereby preventing its complementary pairing with target genes. Compared to miRNA inhibitors, miRNA antagomirs demonstrate greater stability and inhibitory effectiveness in animal studies, and they more easily penetrate cellular membranes and tissue gaps, concentrating in target cells.

mmu-miR-139-3p inhibitor is a complementary single strand fully modified with methoxy to the mature miRNA. This miRNA inhibitor binds specifically to mature miRNA, preventing it from complementary pairing with target genes and thereby inhibiting miRNA function. It is useful for loss-of-function studies of miRNA.

Antibacterial agent 139 exhibits antibacterial activity specifically targeting Gram-positive bacteria, including resistant strains such as MRSA (anti-MRSA), VISA (anti-VISA), and LRSE (anti-LRSE). It operates by depolarizing the bacterial cell membrane [1].

Compound 6h (Anticancer Agent 139) exhibits potent anticancer activity, engaging in a π-cationic interaction with Lys352 of Tubulin and demonstrating high efficacy against SNB-19, OVCAR-8, and NCI-H460 with PGIs of 86.61, 85.26, and 75.99, respectively. Moreover, it shows moderate activity against a range of other cancer cell lines — HOP-62, SNB-75, ACHN, NCI/ADR-RES, 786-O, A549/ATCC, HCT-116, and MDA-MB-231 — with PGIs between 51.88 and 67.55 [1].

[Leu144,Arg147]-PLP (139-151) is a mutated fragment of the myelin proteolipid protein (PLP), featuring substitutions of tryptophan to leucine and histidine to arginine at positions 144 and 147, respectively. Immunizing mice with this peptide (50 µg) mixed in complete Freund's adjuvant (CFA) elevates IL-4 levels in the spleen. While it suppresses Th1 cell activation in vitro, it does not do so in vivo; instead, it promotes the development of regulatory T cells. Preimmunization with [Leu144, Arg147]-PLP (139-151) postpones the onset of experimental autoimmune encephalomyelitis (EAE) triggered by encephalitogenic peptides from PLP (178-191), myelin oligodendrocyte glycoprotein (MOG) (92-106), or myelin basic protein (MBP) in mice.

[Gln144]-PLP(139-151) is an experimental antigen employed to investigate the cross-reactivity of T cells to self and non-self antigens. It activates T cells by binding to the T-cell Receptor (TCR), initiating an immune response. It is useful in the study of autoimmune disease regulation.

E3 Ligase Ligand-linker Conjugate 139 is an E3 ubiquitin ligase ligand and linker for PROTACKB03-SLF, used in cancer research.

SMW139 is a selective allosteric antagonist of the P2X7 receptor, exhibiting a Ki value of 32 nM for human P2X7R. In rat liver microsomes, its half-life is 47 minutes. SMW139 is applicable in research related to inflammation, Alzheimer's disease, and multiple sclerosis.

FGA139 is an inhibitor of cysteine proteases, specifically targeting cathepsin B and L with IC50 values of 4.98 μM and 3.14 μM, respectively. It reduces the production of NO in LPS-induced RAW264.7 cells and lowers TNFα levels in microglia, demonstrating antioxidant and anti-inflammatory properties. Additionally, FGA139 enhances the secretion of neuroprotective metabolites such as purines and linoleic acid in LPS-stimulated microglia. This compound is applicable in the study of neuroinflammatory diseases.

mmu-miR-139-3p Agomir is a specially chemically modified miRNA mimic, featuring methoxy modifications across the full length of the mature miRNA chain, with 2 and 4 thiophosphate linkages at the 5' and 3' ends, respectively, and a high-affinity cholesterol modification attached at the 3' end. This miRNA agomir mimics endogenous miRNA and enhances miRNA activity. Compared to regular mimics, miRNA agomirs show increased stability and inhibitory effects in animal experiments, and they more effectively penetrate cell membranes and tissue gaps to accumulate in target cells.

mmu-miR-139-3p mimic is a chemically synthesized miRNA analogue that simulates endogenous miRNA to enhance miRNA activity for gain-of-function research.

PU139 is a novel inhibitor of histone acetyltransferase (HAT).

Plp(139-151) trifluoroacetate is a useful organic compound for research related to life sciences and the catalog number is T64674.

DK-139 is an inhibitor of NF-kappaB-mediated GROalpha expression, suppressing the TNFalpha-induced invasive capability of MDA-MB-231 human breast cancer cells.

WRR139 is a peptide vinyl sulfone derivative that acts as a potent inhibitor of cytosolic N-glycanase 1 (NGLY1) and the transcription factor Nrf1. NGLY1-mediated deglycosylation is essential for the maturation and activation of Nrf1. By inhibiting NGLY1, WRR139 impairs Nrf1 processing, localization, and activation, thereby suppressing the compensatory expression of proteasome genes. WRR139 significantly potentiates the cytotoxicity of Carfilzomib against cancer cells, serving as a valuable tool for studying proteostasis and overcoming resistance to proteasome inhibitors.

GPR139 agonist-2 (compound 20a), a potent GPR139 agonist with an EC50 of 24.7 nM, has demonstrated efficacy in rescuing social interaction deficits and alleviating cognitive deficits in murine schizophrenia models, indicating its potential in antischizophrenia drug research [1].

AP-4-139B is a potent inhibitor of Heat Shock Protein 70 (HSP70), with an IC50 value of 180 nM. HSP70 is a protein that is overexpressed in various cancers and plays a critical role in the survival and proliferation of tumor cells. AP-4-139B demonstrates significant cytotoxicity in tumor cells, particularly in colorectal cancer cells, making it useful for cancer research.