jnk

JNK Inhibitor VIII (TCS JNK 6o) is an ATP-competitive, selective inhibitor of c-Jun N-terminal kinase (JNK) with IC50 values of 45 nM for JNK-1 and 160 nM for JNK-2.

SP600125 (JNK Inhibitor II) is a JNK inhibitor that inhibits JNK1, JNK2, and JNK3 (IC50=40 40 90 nM) with oral potency, reversibility, and ATP-competitive properties. SP600125 inhibits autophagy and induces apoptosis.

(E)-Ferulic acid methyl ester (Methyl (E)-ferulate) is a potential inhibitor of the mitogen-activated phosphor kinase pathway and an anti-inflammatory agent first isolated from the medicinal plant S. tuberosa. Additionally, it shows promising anthelmintic activity against Haemonchus contortus.

(-)-Bornyl acetate (L-(-)-Bornyl acetate) is a less active enantiomer of (+)-Bornyl acetate. Isolated from hyssop oil, it possesses antifungal, highly active whitening, and antioxidant properties, and it has potential applications in cosmeceutical materials. It downregulates proinflammatory cytokines in vitro and in vivo, reduces the number of total cells, neutrophils, and macrophages in BALF, attenuates histologic lung alterations, decreases the wet-to-dry weight ratio in BALF, and inhibits the activation of NF-kappa-B inhibitor alpha, extracellular regulated protein kinases, c-JunN-terminal kinase, and p38 mitogen-activated protein kinase.

DB07268 is a potent and selective JNK1 inhibitor. It exhibits a strong affinity for the JNK1 enzyme, effectively inhibiting its activity and providing potential therapeutic benefits in conditions where JNK1 is implicated. This compound has demonstrated selective binding to JNK1 over other kinases, underscoring its specificity and promising application in targeted therapies.

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-IN-21 (Compound 62) is an inhibitor of JNK-1.

JNK-IN-22 (Compound 58) is a JNK-1 inhibitor.

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.

IQ-1S free acid (IQ-1S) is an effective and specific c-Jun N-Terminal Kinase Inhibitor. IQ-1S inhibits murine delayed-type hypersensitivity. IQ-1S can reduce inflammation and cartilage loss associated with CIA and can serve as a small-molecule modulator for mechanistic studies of JNK function in rheumatoid arthritis. IQ-1S is highly specific for JNK and that its neutral form is the most abundant species at physiologic pH.

Vincristine binds to tubulin and inhibits the formation of microtubules, thereby inhibiting mitosis of the cancer cell. Vincristine can be used as a microtubule-destabilizing agent for research on the treatment of hematologic cancers, such as leukemia and

1. beta-Asarone (Cis-Isoelemicin) may be a potential preventive drug for Alzheimer's disease. 2. Beta-Asarone prevents autophagy and synaptic loss by reducing ROCK expression in SAMP8 mice. 3. The co-administration of beta-Asarone(Cis-Isoasarone) and l-dopa may contribute to the treatment of 6-OHDA-induced damage in rats by inhibiting autophagy activity. 4. Beta-Asarone exhibits anti-inflammatory effects by suppressing the production of pro-inflammatory mediators through NF-κB signaling and the JNK pathways in activated microglial cells and might be developed as a promising candidate to treat various neuroinflammatory diseases.

Anisomycin is an antibiotic and protein synthesis inhibitor produced by Streptomyces griseolus. It is also a classic activator of p38 MAPK and JNK. By inhibiting protein synthesis, anisomycin induces cellular stress, which activates upstream kinases and subsequently leads to the phosphorylation and activation of p38 MAPK and JNK.

Actein has a stimulatory effect on osteoblastic bone formation or has potential activity against osteoporosis, it also can prevent oxidative damage to osteoblasts in osteoporotic patients. Actein's ability to pathways involved in lipid disorders and carci

JNK-IN-12 (compound P2) is a mitochondrial-targeted JNK inhibitor with an IC50 value of 66.3 nM, consisting of a mitochondrial-specific cell-penetrating peptide linked to SP600125, a selective JNK inhibitor. It selectively impedes mitochondrial JNK phosphorylation without inhibiting nuclear JNK signaling and has shown efficacy in ameliorating Parkinson's disease (PD) symptoms in both in vitro and in vivo studies [1].

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].

JNK-IN-14 is a potent inhibitor of JNK with IC50 values of 1.81 nM for JNK1, 12.7 nM for JNK2, and 10.5 nM for JNK3. It induces early-stage apoptosis, arrests cell population at the G2 M phase, and moderately inhibits beclin-1 production in K562 leukemia cells, demonstrating greater inhibitory efficacy than SP600125. [1]

IQ3 is a selective inhibitor of JNK3(JNK3, JNK1 and JNK2 with Kd of 66 nM, 240 nM and 290 nM, respectively). IQ 3 inhibits NF-κB AP1 transcriptional activity in THP1-Blue cells with IC50 of 1.4 μM, also inhibits TNF-α and IL-6 production in vitro.

Arjunolic acid has antioxidant, anti-inflammatory, antinociceptive and anticholinesterasic (AChE and BuChE) activities, it may as promising targets for the development of innovative multi-functional medicines for Alzheimer desease treatment.

Chrysosplenol D, an efflux pump inhibitor that can potentiate the activity of commercially important antibiotics and antimalarials.

Decursinol angelate has anti-tumor, anti-inflammatory, anti-oxidant, and hepatoprotective activities, it inhibits VEGF-induced angiogenesis via suppression of the VEGFR-2-signaling pathway; it also suppresses invasion and inflammatory activation of cancer

Gartanin is an androgen receptor degradation enhancer, it is also a potential neuroprotective agent against glutamate-induced oxidative injury partially through increasing Nrf-2-independed HO-1 and AMPK/SIRT1/PGC-1α±signaling pathways.

Glycycoumarin is an estrogen agonist, it shows moderate inhibitory effects against CYP1A2 and CYP2B6.