jnk

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.

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.

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.

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.

TCS JNK 5a (SC202671) is an effective, specific inhibitor of JNK3(pIC50= 6.7), JNK2(pIC50=6.5).

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-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-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]

JNK-IN-13 is a selective and potent JNK inhibitor that inhibits JNK3 and JNK2 and can be used in the study of diabetes, inflammation, and neurological disorders.

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.

JNK3 Inhibitor-3 (compound 15g) is a selective, blood-brain barrier permeable, and orally active inhibitor of c-Jun N-terminal kinase 3 (JNK3) with IC50 values of 147.8 nM, 44.0 nM, and 4.1 nM against JNK1, JNK2, and JNK3, respectively. This compound has been shown to significantly enhance memory in mouse models of dementia and is utilized in Alzheimer’s disease research [1].

JNK2-IN-1 (Compound J27), a selective JNK2 inhibitor with a dissociation constant (Kd) of 79.2 µM, exhibits anti-inflammatory effects by attenuating TNF-α and IL-6 secretion via inhibition of the NF-κB/MAPK pathway. It effectively mitigates symptoms associated with LPS-induced acute lung injury (ALI) and sepsis [1].

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

SP 600125, negative control is a methylated analog of SP 600125 and can be used as a negative control for SP 600125. SP 600125, negative control inhibits DTP3 and GADD45β/MKK7 (growth arrest and DNA damage-inducible β/mediator-activated protein kinase kinase kinase 7) and is capable of restoring activation.The IC50s of SP 600125, negative control against JNK2 and JNK3 were 18 and 24 μM, respectively.

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.

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.

Urolithin B is one of the gut microbial metabolites of ellagitannins and is found in diverse plant foods, including pomegranates, berries, walnuts, tropical fruits, and medicinal herbs. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. Urolithin B has anti-inflammatory and antioxidant effects.

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

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.

(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.

AS601245.2TFA (345987-15-7 free base) (AS601245.2TFA) is a cell-permeable Inhibitor of JNK (IC50s of 150, 220, and 70 nM for hJNK1, hJNK2, and hJNK3, respectively).

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

Apelin-12 acetate possesses a high affinity to orphan receptor APJ receptor. Apelin-12 acetate inhibits the JNK and p38 MAPK signaling pathway of the apoptosis-related MAPKs family, thus offering protection to neurons.

Epieriocalyxin A can suppress Caco-2 colon cancer cell growth. It could be a potential drug for colon cancer therapy in the future.

JIP-1 (153-163) acetate(438567-88-5 free base) is a peptide inhibitor of c-Jun N-terminal kinase (JNK), based on residues 153-163 of JNK-interacting protein-1 (JIP-1). JIP-1 (153-163) acetate(438567-88-5 free base) binds to JNK with affinity in the micromolar range and minimally inhibits p38 and ERK.

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

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

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.

D-JNKI-1 (AM-111) is a highly effective, cell-permeable peptide inhibitor.

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

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.

TAK-715 is a p38 MAPK inhibitor for p38α.

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.

WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of new therapeutics.

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

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.

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.

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

d-Epigalbacin ((-)-Zuonin A) is a naturally occurring lignin. d-Epigalbacin is a potent, selective JNKs inhibitor, with IC50s of 1.7 μM, 2.9 μM and 1.74 μM for JNK1, JNK2 and JNK3, respectively.

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

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.

Panaxydol has anti-cancer activity, can inhibit the growth and apoptosis of cancer cells, the signaling mechanisms involve a [Ca(2+)](i) increase, JNK and p38 MAPK activation, cAMP, MAP kinase and ROS generation through NADPH oxidase and mitochondria.

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

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.

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

N-Butyl α-D-fructofuranoside, extracted from the root barks of Ulmus davidiana var. japonica, amplifies Nrf2 activity via JNK activation and exhibits anti-inflammatory properties [1] [2].

Phytolaccaceae has anti-tumor activity, the mechanism may be related to the capacity of Esculentoside H for TNF release.

Theobromine (3,7-Dimethylxanthine), a xanthine alkaloid, is used as a bronchodilator and as a vasodilator.