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.

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.

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, a peptide vinyl sulfone, plays a role in disease processes including inflammation and cancer, and acts as an inhibitor of cytosolic enzyme N-glycanase 1 (NGLY1) and Nrf1. Moreover, WRR139 amplifies the cytotoxic effects of Carfilzomib on cancer cells [1].

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.

PLP (139-151) is an amino acid fragment from positions 139 to 151 of myelin proteolipid protein (PLP), which is used to induce the relapsing-remitting experimental autoimmune encephalomyelitis (RR-EAE) model.

[SER140]-PLP(139-151) is a polypeptide fragment derived from the myelin-associated lipid protein.

[SER140]-PLP(139-151) acetate is a peptide fragment from myelin proteolipid protein (PLP).

[SER140]-PLP(139-151) (TFA) is a polypeptide fragment of the myelin lipid protein.

[L144-PLP(139-151)], a peptide ligand of the T cell receptor (TCR), acts as a TCR antagonist specifically inhibiting the activation of encephalitogenic Th1 clones [1].