JNJ-42165279 is a fatty acid amide hydrolase (FAAH) inhibitor developed by Janssen Pharmaceutica and IC50 value is 70 nM. It is described as a covalently binding but slowly reversible selective inhibitor of FAAH. Phase II human trials for the treatment of anxiety disorders and major depressive disorder is on-going.
JNJ-26483327 is an orally bioavailable, small-molecule, multitargeted reversible tyrosine kinase inhibitor with potential antineoplastic activity. Multitargeted tyrosine kinase inhibitor JNJ-26483327 binds to and inhibits several members of the epidermal growth factor receptor (EGFR) family, including EGFR, HER2 and HER4; Src family kinases (Lyn, Yes, Fyn, Lck and Src); and vascular endothelial growth factor receptor type 3 (VEGFR3). By inhibiting several different signaling molecules that play crucial roles at various stages in tumorigenesis, this agent may inhibit tumor growth, invasion, migration and metastasis. In addition, JNJ-26483327 crosses the blood-brain barrier (BBB).
JNJ 63533054 is a potent and selective GPR139 agonist (EC50 = 16 nM) that is brain and cell penetrant. JNJ 63533054 is selective for GPR139 over a panel of GPCRs, ion channels and transporters, including GPR142.
JNJ 0966 is a selective inhibitor of MMP-9 (IC50 = 440 nM) with no effect on MMP-1, MMP-2, MMP-3, MMP-9, or MMP-14 catalytic activity. JNJ 0966 was indicated to alleviate the pain of experimental autoimmune encephalomyelitis in a mouse model.
JK-P3 is a VEGFR2 inhibitor with IC50 values of 7.8 μM. JK-P3 inhibits FGFR 1/3 kinase activity in vitro, but exhibits no effect on FGFR signaling in cell-based assays. It suppresses wound healing and tube formation in HUVEC without effecting endothelial cell proliferation.
JK-184 is a potent downstream hedgehog (Hh) signaling antagonist that functions by alcohol dehydrogenase 7 (Adh7) inhibition, preventing Gli-dependent transcriptional activity (IC50 = 30 nM). Hedgehog signaling plays a key role in a wide variety of developmental processes as well as cancer progression. JK-184 exhibits antiproliferative activity.
JHU37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist. It has high affinity in vitro for hM3Dq and hM4Di (Ki values are 1.9 nM (hM3Dq) and 3.6 nM (hM4Di).
Jervine is a naturally occuring steroidal alkaloid that causes cyclopia by blocking sonic hedgehog(Shh) signaling. It is an inhibitor of Smo and derived from the Veratrum plant species. Jervine can be used to induce abnormal morphogenesis in a number of experimental models.
JE-2147 is a dipeptide HIV protease inhibitor (PI) that is effective against a wide spectrum of HIV-1, HIV-2, simian immunodeficiency virus, and various clinical HIV-1 strains in vitro.
Jd-5037 is a peripherally-restricted cannabinoid inverse agonist at CB1 receptors that can be used as an anti-obesity drug, with a 700-fold higher affinity compared to CB2 receptors.
Jatrorrhizine Hydrochloride (JH), an active component of the traditional Chinese medicinal herb Coptis chinensis, inhibited the proliferation and neovascularization of C8161 human metastatic melanoma cells. The effective inhibitory effects of Jatrorrhizine Hydrochloride on metastatic melanoma cell proliferation and neovascularization with low toxicity suggest that Jatrorrhizine Hydrochloride is a potential new antimelanoma drug candidate.
A cell-permeable, reversible, potent, ATP-competitive, and specific inhibitor of JAK3 (Janus family kinase 3; IC50 = 78 µM). Has no effect on JAK1, JAK2, or Zap/Syk or Src tyrosine kinases. Acts as a potent inhibitor of glioblastoma cell adhesion and migration. Also reported to block thrombin-induced platelet aggregation.
J 147, under the IUPAC name N-(2,4-dimethylphenyl)-2,2,2-trifluoro-N-[(E)-(3-methoxyphenyl)methylideneamino]acetamide, is a phenyl hydrazide compound that has been shown to prevent memory deficits in an Alzheimer's disease mouse model. in vitro: A potent neuroprotective and neurotrophic compound (EC50 = 25 - 200 nM) in vivo: Reduces soluble Aβ40 and Aβ42 levels and increases BDNF levels in the hippocampus
Ixabepilone (also known as azaepothilone B, or BMS-247550) is an orally bioavailable microtubule inhibitor. Ixabepilone was a semisynthetic analogue of epothilone B with antineoplastic activity. Ixabepilone binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis. This agent demonstrates antineoplastic activity against taxane-resistant cell lines. Ixabepilone was approved in 2007.
IXA4 is a highly selective and non-toxic IRE1/XBP1s activator, which activates the IRE1/XBP1s signaling, regardless of the global activation of the unfolded protein response (UPR) or other stress-responsive signaling pathways, such as heat shock response or oxidative stress response. IXA4 reduces APP secretion by activating IRE1. IXA4 therapy improves systemic glucose metabolism and hepatic insulin action through IRE1-dependent liver transcriptomic remodeling, thereby reducing glucose production and steatosis. IXA4-stimulated IRE1 activation also enhances pancreatic function.
Ivosidenib is an oral inhibitor that specifically inhibits a mutated form of IDH1 in the cytoplasm, which blocks the proliferation of tumor cells expressing IDH1.
Ivacaftor is a potentiator of CFTR targeting G551D-CFTR(EC50=100 nM)and F508del-CFTR(EC50=25 nM). Ivacaftor is used in the treatment of cystic fibrosis.
The enantiomer of Ivabradine Hydrochloride. Ivabradine is a medication used to reduce the risk of hospitalization for worsening heart failure in adult patients with stable, symptomatic chronic heart failure.
An impurity of Ivabradine, which is a novel heart rate lowering medication. It can slow the heart rate by hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blockers. Ivabradine is marketed under trade names including Coralan, Corlentor, Procoralan, Coraxan.
ITI214 is a highly selective PDE1 inhibitor (Ki = 58 pM) at picomolar concentration without disrupting other PDE family members and a panel of enzymes, receptors, transporters, and ion channels.
IT 901, a bioactive naphthalenethiobarbiturate derivative, potently inhibits the NF-κB subunit c-Rel with IC50 value of 3 μM. It shows its anticancer properties in Hematologic Malignancies by inhibiting the oxidative stress response in lymphoma cells. It suppressed graft-versus-host disease while preserving graft-versus-lymphoma activity during allogeneic transplantation. It did not elicit increased levels of reactive oxygen species in normal leukocytes, illustrating its cancer selective properties. It is used for the treatment of human B-cell lymphoma and reveals antitumor properties in vitro and in vivo. It is also a novel therapeutic agent to ameliorate graft-versus-host disease.
Ispinesib is a synthetic small molecule, derived from quinazolinone, with antineoplastic properties. Ispinesib selectively inhibits the mitotic motor protein, kinesin spindle protein (KSP), resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest during the mitotic phase, and cell death in tumor cells that are actively dividing. Because KSP is not involved in nonmitotic processes, such as neuronal transport, ispinesib may be less likely to cause the peripheral neuropathy often associated with the tubulin-targeting agents.
Isoscoparin is a compound of the flavonoid class found in the seeds of Alliaria petiolata with antioxidant activity. Isoscoparin is promisingly used in the treatment of obesity for its anti-adipogenic property.
Isorhamnetin-3-O-galactoside, an indigenous flavonoid constituent obtained through extraction from spinach and onions, has been documented to exhibit substantial antioxidative and anti-inflammatory properties, evincing prospects as a therapeutic agent in diverse ailments encompassing malignancy, diabetes, and Alzheimer's.
Isopropyl 4-[4-[N,N-bis(2-hydroxyethyl)amino]phenyl]butyrate, a pharmaceutical intermediate, can be utilized in the production of drugs intended for the treatment of cardiovascular disease, such as hypertension. It functions as an angiotensin-converting enzyme (ACE) inhibitor, which reduces the likelihood of heart attack and stroke by regulating blood pressure levels. Consequently, it plays a valuable role in managing these serious medical conditions, thus improving overall health outcomes among patients.
Isomogroside V is extracted from the fruit of Siraitia grosvenorii Swingle. It was determined to be approximately 500 times sweeter than 0.5% (w/v) sucrose.
Isoliensinine, a natural phenolic bisbenzyltetrahydroisoquinoline alkaloid, has received considerable attention for its potential biological effects such as antioxidant and anti-HIV activities. It possesses an anti-proliferative effect, which is related to the decrease of the overexpression of growth factors PDGF-beta, bFGF, proto-oncogene c-fos, c-myc and hsp70.
Isoindigotin is a natural product found in Isatis tinctoria. Isoindigotin is an electron-accepting building block for the preparation of electroactive materials for organic electronics.
