nk-1

NKP608 is a selective and highly effective neurokinin-1 (NK-1) receptor antagonist with anticancer and antianxiety activities, inhibiting the proliferation of human colorectal cancer cells through the Wnt signaling pathway.

NK-1 Antagonist 1 is a NK-1 receptor antagonist.

JNK-1-IN-3 (Compound 9e) acts as a JNK1 inhibitor, both reducing JNK1 gene expression and lowering the protein levels of its phosphorylated form. It concurrently diminishes the expression of downstream targets c-Jun and c-Fos in tumors, while also restoring p53 activity. Exhibiting broad-spectrum antiproliferative effects, JNK-1-IN-3 is particularly effective against renal and breast cancer cell lines, showing significant anticancer activity both in vivo and in vitro.

JNK-1-IN-4 (Compound E1) is an inhibitor of JNK, targeting JNK-1, JNK-2, and JNK-3 with IC50 values of 2.7, 19.0, and 9.0 nM, respectively. This compound inhibits the phosphorylation of c-Jun and reduces the expression of TGF-β1-induced EMT markers (such as fibronectin and α-SMA). JNK-1-IN-4 exhibits favorable pharmacokinetic properties with a bioavailability of 69%. Additionally, it demonstrates antifibrotic effects in a Bleomycin-induced mouse model of idiopathic pulmonary fibrosis.

JNK-1-IN-5 (Compound 14) is a potent JNK1 inhibitor with sub-nanomolar efficacy. It effectively inhibits TGF-β-induced epithelial-mesenchymal transition and shows promise for research targeting JNK1 as an anti-pulmonary fibrosis agent.

Nk-1145 is a parasympathetic drug of the autonomic nervous system, which can cause behavioral stimulation and excitement.

NK-122 is a potential bioactive agent. No further details yet.

JNK-1-IN-1 is an inhibitor specifically targeting JNK-1, also exhibiting inhibition of MKK7 with an IC50 value of 7.8μM. It binds to MKK7cp, further reinforcing its role as a JNK-1 inhibitor.

JNK-1-IN-2 (Compound c6) is a potent inhibitor of JNK-1 with an IC50 of 33.5 nM, and also exhibits inhibitory effects on JNK-2 and JNK-3 with IC50 values of 112.9 nM and 33.2 nM, respectively. This compound effectively inhibits the phosphorylation of c-Jun and has shown potential in reversing lung impairment, making it relevant for research into pulmonary fibrosis [1].

Ponatinib, also known as PonatiLink-1-24, is a selective inhibitor of the Abelson murine leukemia (ABL) enzyme [1].

DosatiLink-1 acts as an inhibitor of the Abelson murine leukemia (ABL) enzyme [1].

Rapalink-1 is a brain-permeable mTOR inhibitor that inhibits oxidative stress-induced DNA damage and senescence in ethanol-exposed endothelial cells, and inhibits the mTORC1-4E-BP1 pathway in mice.Rapalink-1 is used for the study of prostate cancer due to its anticancer activity.

MEN11467 is a novel, orally available, potent and selective peptidomimetic tachykinin NK 1 receptor antagonist for the study of acute colon cancer.

Burapitant (SSR 240600) is a novel non-peptide tachykinin neurokinin 1 (NK) receptor antagonist with anti-coke oven and antidepressant activity.

Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).

Vofopitant dihydrochloride (GR 205171A) is an orally available, selective tachykinin NK1 receptor antagonist that inhibits [3H]SP binding to NK1 with pKi values of 9.5 and 10.6, respectively. It is a potential compound for the treatment of pathological vomiting.

Lanepitant 2HCl is a non-peptide neurokinin-1 receptor antagonist with analgesic and anti-inflammatory activity.Lanepitant 2HCl inhibits the binding of Substance P to the neurokinin-1 receptor, inhibits neurogenic inflammation and pain transmission, and can be used in the study of painful neuropathic disorders, such as migraines.

WIN 51,708 is a neurokinin receptor (NK1) antagonist.

Ezlopitant (CJ-11974) is a small molecule neurokinin-1-receptor (NK1) antagonist used to treat nausea, vomiting and pain.

(R)-CJ 11974: non-peptide NK1 receptor antagonist, may relieve pain and prevent chemo-induced vomiting.

Aprepitant is a Substance P/Neurokinin-1 Receptor Antagonist. The mechanism of action of aprepitant is as a Neurokinin 1 Antagonist, and Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 2C9 Inducer, and Cytochrome P450 3A4 Inducer.

Elinzanetant is a dual antagonist of neurokinin (NK) receptors 1 and 3 and modulates reproductive hormone secretion.

L-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM)

[Sar9]-Substance P acetate is one of NK-1 receptor agonist. The action of SP on progesterone metabolism was mimicked by the rNK1-specific agonist [Sar-9,Met(O2)11]-SP.