JNK

JNK-IN-11 is a potent JNK inhibitor that inhibits JNK1, JNK2, and JNK3 with IC50 values of 1.8, 21.4, and 2.2 µM, respectively.JNK-IN-11 can be used to study abnormalities in immune function.

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). The selectivity is higher 10-fold than MNK2, Fms and no inhibition of Met, c-Kit, PDGFRβ in A375 cell line.

JNK-IN-12 (compound P2) is a mitochondrial-targeted JNK inhibitor with an IC50 value of 66.3 nM, comprising 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 been shown to ameliorate Parkinson's disease (PD) symptoms in both in vitro and in vivo studies [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.

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

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-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]

TOPK-p38/JNK-IN-1 (Compound B12) is an orally active inhibitor of the TOPK-p38/JNK signaling pathway, with an IC50 value of 2.14 μM for the inhibition of NO production. It demonstrates anti-inflammatory properties by inhibiting downstream phosphorylation of related proteins and preventing the degradation of TOPK [1].

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.

Akt/NF-κB/JNK-IN-1 (Compound 2i) is an inhibitor of Akt, NF-κB and JNK signalling pathways.Akt/NF-κB/JNK-IN-1 exhibits an inhibitory effect on nitric oxide production (IC50: 3.15 μM) and shows anti-inflammatory effects.

JNK3 Inhibitor-4, a potent 2-aryl-1-pyrimidinyl-1H-imidazole-5-yl acetonitrile derivative, demonstrates a strong inhibitory effect on JNK3 with an IC 50 value of 1.0 nM. It exhibits exceptional selectivity against JNK3 when compared to other protein kinases, including isoforms JNK1 (IC 50 = 143.9 nM) and JNK2 (IC 50 = 298.2 nM). Additionally, JNK3 Inhibitor-4 benefits from neuroprotective properties and is predicted to permeate the blood-brain barrier effectively.

JNK3 inhibitor-1 is a highly potent and selective compound that specifically inhibits JNK3 with an impressive IC50 value of 0.005 μM. In addition to its remarkable inhibitory effects, JNK3 inhibitor-1 possesses excellent oral bioavailability and the ability to efficiently penetrate the brain.

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].

JNK3 Inhibitor-8 is a potent, selective, and orally active inhibitor that can cross the blood-brain barrier, targeting JNK3 with IC50 values of 21 nM for JNK3, 2203 nM for JNK2, and >10000 nM for JNK1. This compound demonstrates significant neuroprotective effects and holds promise for Alzheimer’s disease (AD) 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].

JNK3 inhibitor-7, a potent and orally active compound that can cross the blood-brain barrier, acts as a JNK3 inhibitor with IC50 values of 53 nM for JNK3, 973 nM for JNK2, and 1039 nM for JNK1. Demonstrating significant neuroprotective effects, JNK3 inhibitor-7 holds potential for Alzheimer’s disease (AD) research [1].

JNK3 inhibitor-2 is a potent and selective JNK3 inhibitor. The IC50 values of JNK3 inhibitor-2 for JNK1, JNK2, JNK3 are >100, >100, 0.25 μM, respectively. JNK3 inhibitor-2 also inhibits DDR1 and EGFR (T790M, L858R) [1].

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.

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.

SR-3306 is a potent and highly inhibitor of brain penetrant JNK.

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.

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.

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

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.

CP-380736 (PF-00520893) is an epidermal growth factor receptor (EGFR) inhibitor. EGFR is a tyrosine kinase that activates MAPK, JNK, and Akt pathways, and is an important mediator of several types of cancer.

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

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.

Mefloquine (Ro 215998), a quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus, and cancer research.

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.

RAPTA-C induces EAC cell cycle arrest and apoptosis via the mitochondrial and p53-JNK pathways, and can be used in the study of breast and ovarian cancer.

SF5 is an inhibitor of the apoptosis pathway. Which is through the JNK-p53-caspase apoptotic cascade.

TASIN-1 Hydrochloride (TASIN-1 HCl) is a selective inhibitor of truncated APC that acts by selectively killing colorectal cancer cells that express truncated APC by reducing cellular cholesterol levels and inducing apoptotic cell death through the ER stress ROS JNK signaling in colon cancer cells.

TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1)(IC50 of 14 nM).

NSC-697923 (2-[(4-methylphenyl)sulfonyl]-5-nitrofuran), a potent inhibitor of UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13), exhibits its role in inducing cell death in neuroblastoma (NB) cells through two distinct mechanisms. In p53 wild-type NB cells, NSC-697923 promotes the nuclear importation of p53, thereby triggering cell death. Meanwhile, in p53 mutant NB cells, NSC-697923 activates the JNK-mediated apoptotic pathway, leading to cell death. Additionally, NSC-697923 inhibits DNA damage and NF-κB signaling, further contributing to its antitumor activity.

L-JNKI-1 is a cell-permeable peptide inhibitor specific for JNK, it has been shown to effectively inhibit JNK activity in in vivo studies.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK/p38 MAPK signaling pathways in the murine macrophages.

Taurochenodeoxycholic Acid (12-Deoxycholyltaurine) is one of the main bioactive substances of animals' bile acid.

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

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

10-Gingerol-induced apoptosis was accompanied by phosphorylation of the mitogen-activated protein kinase (MAPKs) family, p38 MAPK (p38), c-Jun N-terminal kinase (JNK), and extracellular signal-regulated kinase (ERK).

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.

Lawsone methyl ether (2-Methoxy-1,4-naphthoquinone) induced apoptosis of A549 cells independent of cell cycle arrest, and is mediated by the JNK and p38 MAPK signaling pathways. Further analysis demonstrated that these signaling pathways were stimulated by oxidative DNA damage caused by increased ROS generation in MNQ-treated A549 cells.

Icaritin (Anhydroicaritin) has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apoptosis, inhibit ENKL cell proliferation. Icaritin has anti-multiple myeloma activity, mainly mediated by inhibiting IL-6/JAK2/STAT3 signaling. Icaritin at low concentration (4 or 8 μMol/L) can promote rat chondrocyte proliferation and inhibit cell apoptosis, while the effect of Icaritin on rat chondrocyte at high concentration was reversed.

CAY10594 is a potent phospholipase D2(PLD2) inhibitor. CAY10594 ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β JNK axis.

Chloramphenicol (Chloromycetin), a broad-spectrum antibiotic, blocks bacterial protein synthesis.

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