jnk 3

JNK-1-IN-3 (Compound 9e) is a JNK1 inhibitor that downregulates JNK1 and phosphorylated JNK1, reduces c-Jun and c-Fos expression in tumours, and restores p53 activity. JNK-1-IN-3 exhibits potent antiproliferative activity against renal carcinoma and breast cancer cell lines.

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.

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.

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

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 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.

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.

AMG-548 is a selective and orally active p38α MAPK inhibitor (Ki = 0.5 nM), with higher selectivity than p38β, p38γ, and p38δ, and can also inhibit the TNFα, CK1δ/ε, and Wnt signalling pathways.

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.

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

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.

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.

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.

TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM.TA-02 especially inhibits TGFBR-2.

JTP10-△-R9 TFA is a selective inhibitor of the JNK2 peptide (IC50: 89 nM), demonstrating 10-fold higher selectivity for JNK2 over JNK1 and JNK3.

JTP10-△-TATi TFA is a selective inhibitor of JNK2 peptide (IC50: 92 nM), demonstrating 10-fold selectivity for JNK2 over JNK1 and JNK3.

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.

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.

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.

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

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

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.

1. 2,5-Dihydroxyacetophenone (Quinacetophenone) possess anti-anxiety, and neuroprotective qualities. 2. 2,5-Dihydroxyacetophenone (Quinacetophenone) reatment can induce a sustained activation of JNK, ERK1/2, and p38 MAPKs, it also can potentiate the pro-apoptotic and anti-proliferative effects of bortezomib in U266 cells. 3. 2,5-Dihydroxyacetophenone (Quinacetophenone) has anti-inflammatory activity in activated macrophages, raising the possibility that this compound has a therapeutic potential for inflammatory conditions. 4. 2,5-Dihydroxyacetophenone (Quinacetophenone) is an uncompetitive inhibitor of murine tyrosinase (K(I) 0.28mm), it strongly inhibits both melanogenesis and cellular tyrosinase activity in vitro in 3-isobutyl-1-methylxanthin-stimulated B16 mouse melanoma cells or in vivo in zebrafish and mouse models.