JNK

SKLB-163 acts by downregulating RhoGDI, activating JNK-1 signaling pathway and caspase-3, and reducing phosphorylated Akt and p44/42 MAPK.

SR-3306 is a brain-penetrant and selective pan-JNK (JNK1 2 3) inhibitor with IC50 values ​​of 67 nM, 283 nM, 159 nM, respectively, and reduces food intake and body weight.

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

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

N-Methylnicotinamide is one of the endogenous metabolites that ameliorates endothelial dysfunction.

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.

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

Anisomycin (NSC-76712) is an antibiotic isolated from various Streptomyces species. It interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system.

D-JNKI-1 acetate (AM-111 acetate) is a highly potent and cell-permeable peptide inhibitor of JNK.

Tanzisertib (CC-930) (CC-930) is a potent inhibitor of JNK1 2 3 with IC50s of 61 7 6 nM, respectively, with potential antifibrotic activity.

JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1 2 4 inhibitor (IC50: 4.7 18.7 1 nM) with over 10-fold selectivity compared to MNK2 and Fms, and no inhibition of Met, c-Kit, or PDGFRβ in the A375 cell line.

Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.

Astragaloside IV (AS-IV), an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1 2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine.1 It dose-dependently inhibits human adenovirus type 3 (HAdV-3) in A549 cells (IC50 = 23 μM; LC50 = 865 μM).It inhibits replication of HAdV-3 and decreases HAdV-3-induced apoptosis. It has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems. In particular, it reduces myocardial infarct size in dogs when administered prior to coronary ligation and reduces reperfusion arrhythmias in isolated rat hearts.

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.

Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.

Guggulsterone (Guggulsterone E&Z) E&Z is a 3-hydroxy steroid. It has a role as an androgen.

JNK-IN-7 (JNK inhibitor) is a selective JNK1 2 3 inhibitor (IC50: 1.54 1.99 0.75 nM). It can also inhibit phosphorylation of c-Jun, which is a substrate of JNK kinase.

1. Cornuside (Comuside) has immunomodulatory activity . 2. Cornuside suppresses expression levels of cytokine-induced proinflammatory and adhesion molecules in the human endothelial cells. 3. Cornuside can treat myocardial I R and protect the liver from CCl4-induced acute hepatotoxicity, by reducing oxidative stress and suppressing inflammatory responses. 4. Cornuside has anti-inflammatory activity by downregulations of iNOS and COX-2 due to NF-κB inhibition as well as the negative regulation of ERK1 2, p38, and JNK1 2 phosphorylations in RAW 264.7 cells. 5. Cornuside has protective potential against cerebral ischemic injury, may be due to the suppression of intracellular Ca(2+) elevation and caspase-3 activity, and improvements in mitochondrial energy metabolism and antioxidant properties.

Tomatidine serves as an anti-inflammatory agent by inhibiting NF-κB and JNK signaling pathways. Additionally, it induces autophagy in both mammalian cells and C. elegans.

1. Sesamolin and Sesamin has neuroprotective effect. 2. Sesamolin protects microglia against H2O2-induced cell injury, by inhibiting of p38 MAPK and caspase-3 activation and ROS production. 3. Sesamolin and Sesamin can significantly attenuate the excess g

Juglanin is a JNK activator. Juglanin with inflammation and anti-tumor activities. It can induce apoptosis and autophagy on human breast cancer cells.

Vacquinol-1 is an MKK4 activator, which rapidly and selectively induces glioma cell death.

Ginsenoside Re (Ginsenoside B2) may have properties that inhibit or prevent the growth of tumors.

3',4',7-Trihydroxyisoflavone is a soy isoflavone soy glycoside derivative and Cot (Tpl2 MAP3K8) and MKK4 inhibitor with anticancer, antiangiogenic and free radical scavenging properties.3',4',7-Trihydroxyisoflavone enhances memory effects through modulation of cholinergic function and BDNF signaling pathway in mice.3',4',7-Trihydroxyisoflavone can improve skin barrier function impaired by endogenous or exogenous glucocorticoids and can be used in the study of atopic dermatitis. 3',4',7-Trihydroxyisoflavone enhances memory effects by modulating cholinergic function and BDNF signaling pathway in mice. It can improve the skin barrier function impaired by endogenous or exogenous glucocorticoids, and can be used in the study of atopic dermatitis.

Loureirin B can downregulate the expression of fibrosis-related molecules by regulating MMPs and TIMPs levels, inhibit scar fibroblast proliferation and suppress TGF-β1-induced fibrosis, during which TGF-β1 Smad2 3 pathway is likely involved.

1. Isovitexin (Apigenin-6-C-Glucoside) exhibits a potential antioxidant activity. 2. Isovitexin shows a strong antihyperglycemic action, inhibits α-glucosidase in vivo.

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.

AS601245 is an inhibitor of the c-Jun NH2-terminal kinase (JNK), with neuroprotective properties.

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.

GSK1838705A is an effective IGF-1R inhibitor (IC50: 2.0 nM), modestly potent to IR (IC50: 1.6 nM) and ALK (IC50: 0.5 nM), respectively, and little inhibition to other protein kinases.

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.

BSJ-04-122 is a covalent dual inhibitor of MKK4 and MKK7, demonstrating IC50 values of 4 nM and 181 nM, respectively. [BSJ-04-122] can be used for cancer research.

IRAK inhibitor 1 is an effective IRAK-4 inhibitor (IC50: 216 nM), is poorly active against JNK-1 (IC50: 3.801 μM) and JNK-2 (IC50>10 μM).

CC-401 Hydrochloride (CC401 HCl) is a second generation ATP-competitive anthrapyrazolone c-Jun N terminal kinase (JNK) inhibitor (Ki of 25 to 50 nM.)with potential antineoplastic activity.

Indirubin-3′-oxime is an effective inhibitor of cyclin-dependent protein kinases, and may play an obligate role in neuronal apoptosis in Alzheimer's disease.

SU3327 (halicin) is a potent, selective and substrate-competitive inhibitor of JNK(IC50 of 0.7 μM).

Bentamapimod (AS 602801) is a novel, orally active inhibitor of JNK.

Uvaol is present in olives and virgin olive oil with anti-inflammatory, anti-proliferative, and vasorelaxant activities.

TAK-715 is a p38 MAPK inhibitor for p38α.

CC-90001 is an orally administered c-Jun N-terminal kinase (JNK) inhibitor with bias for JNK1 over JNK2.

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

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

BI-78D3, a competitive JNK inhibitor. IC50 of BI-78D3 is 280 nM that displays > 100 fold selectivity over p38α, and have no activity at mTOR and PI-3K.

Astragaloside, one of the main active ingredients in Astragalus membranaceus.

JNK-IN-11 (compound 1) is a potent inhibitor of JNK, with IC50 values of 2.2 μM, 21.4 μM, and 1.8 μM for JNK1, JNK2, and JNK3, respectively, showing potential for Alzheimer's and Parkinson's disease research.

J30-8 is a subtype-selective and potent JNK3 inhibitor (IC50: 40 nM) with neuroprotective activity for the study of neurodegenerative diseases such as Alzheimer's disease.

Tomatidine hydrochloride (Tomatidine HCl) is a steriodal alkaloid structurally similar to Cyclopamine but does not inhibit hedgehog pathway. May be used as a negative control for Cyclopamine and KAAD-Cyclopamine. Tomatidine protects against muscle atrophy and boosting muscle growth.