j-1

Melflufen (Melphalan flufenamide), a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen exhibits significant antitumor activity against multiple myeloma (MM) cells and has been shown to inhibit angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells, thereby contributing to its antitumor efficacy. At equivalent molar concentrations, both the salt and free forms of Melflufen exhibit comparable biological activity. However, the salt form, Melflufen hydrochloride, typically demonstrates enhanced water solubility and stability, which may contribute to its increased therapeutic potential.

GSK-J1 lithium salt is an effective inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with an IC 50 of 60 nM for KDM6B.

GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, >10-fold selectivity over other tested demethylases.

SIBA (5'-Deoxy-5'-isobutylthioadenosine) is a synthetic analogue of SAH, acts as an inhibitor of S-adenosylmethionine-mediated transmethylation. SIBA can interfere with a variety of enzymatic activities in vitro, such as SAH hydrolase, methylthioadenosine phosphorylase and cAMP phosphodiesterase. SIBA reversibly blocks the multiplication of herpes simplex type 1 virus (HSV)

ADS-J1 is an HIV-1 entry inhibitor that potently inhibits seminal amyloid fibrillization and block fibril-mediated enhancement of viral infection. Semen-derived amyloid fibrils, comprising SEVI (semen-derived enhancer of viral infection) fibrils and SEM1 fibrils, may remarkably enhance HIV-1 sexual transmission and are potential targets for the development of an effective microbicide.

GSK-J1 sodium salt is a potent inhibitor of the H3K27 histone demethylases JMJD3 and UTX.

J-104871 (UNII-6137X5QNJF) is a novel farnesyltransferase (FTase) inhibitor that competitively blocks Ras farnesylation in vivo, inhibits Ras processing in activated H-ras-transformed NIH3T3 cells, and suppresses tumor growth in nude mice transplanted with activated H-ras-transformed NIH3T3 cells.

CJ-13,610 is an orally active and nonredox-type inhibitor of 5-lipoxygenase (5-LOX). CJ-13,610 inhibits the biosynthesis of leukotriene B4 and regulates the expression of IL-6 mRNA in macrophages.

CJ-13,610 hydrochloride is an orally active nonredox-type inhibitor of 5-LOX and can be used in studies about the prevention of untoward pathophysiological effects of LTs.

JNJ-10311795 (RWJ-355871) is a potent dual inhibitor of neutrophil elastase (Ki = 38 nM) and mast cell chymase (Ki = 2.3 nM) with significant anti-inflammatory activity, useful for studying pneumonia.

ZX-J-19J (N-(2,3-Diphenyl-6-quinoxalinyl)octanamide), an inhibitor of Cyclophilin J (CyPJ), demonstrates remarkable inhibition of tumor cell growth, comparable to cyclosporine A but much stronger than 5-fluorouracil.

J-147 is an experimental drug with reported effects against both Alzheimer's disease and ageing in mouse models of accelerated aging. It is a curcumin derivative and a potent neurogenic and neuroprotective drug candidate initially developed for the treatment of neurodegenerative conditions associated with aging that impacts many pathways implicated in the pathogenesis of diabetic neuropathy.

SSJ-183 is a low-toxicity and orally available and anti-malarial drug with an IC50 = 7.6 nM against P. falciparum and no lethality at doses up to 2000 mg/kg po.

JNJ-1661010 (Takeda-25) is an effective and specific FAAH inhibitor (IC50: 10/ 12 nM for rat/human), shows >100-fold selectivity for FAAH-1 than FAAH-2.

J-104132 is a potetn and selective endothelin A/B receptor antagonist (Ki: cloned human ETA = 0.034 nM; cloned human ETB = 0.104 nM) . In vitro, J-104132 is a potent antagonist of ET-1-induced accumulation of [3H]inositol phosphates in Chinese hamster ova

(S,S)-J-113397, an isomer of J-113397, is an opioid receptor antagonist [1].

J-1048, an activin receptor-like kinase 5 (ALK5) inhibitor, effectively suppresses TAA-induced liver fibrosis in mice through specific inhibition of the TGF-β/Smad signaling pathway [1].

Cis-J-113863 is a competitive antagonist for the chemokine receptor 1 (CCR1), demonstrating inhibitory concentration 50 (IC50) values of 0.9 nM for human CCR1 receptors and 5.8 nM for mouse CCR1 receptors, respectively [1].

Trans-J-113863 serves as a potent antagonist of chemokine receptors CCR1 and CCR3, effectively inhibiting MIP-1α-induced chemotaxis in CCR1 transfectants and eotaxin-induced chemotaxis in CCR3 transfectants, with respective half-maximal inhibitory concentrations (IC50) of 9.57 nM and 93.8 nM [1] [2].

J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.

JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist with pKis of 8.19 and 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.

JNJ- 10198409 is a relatively selective and ATP competitive PDGF-RTK inhibitor (IC50=2 nM). JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent.

SJ-172550 is a small molecule inhibitor of MDMX (EC50: 5 μM).

SJ-106C, a SIRT inhibitor, exhibits IC50 values of 0.59, 0.12, and 0.49 μM against SIRT1/2/3, respectively. This compound specifically targets mitochondria and inhibits the growth of DLBCL tumors.