jnk1/2

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.

ZG-10 (JNK-IN-2) is an inhibitor of JNK, blocking JNK1, JNK2, and JNK3, and is used in studies of SARS-CoV-2 virus infection.

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.

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.

3'-Hydroxypterostilbene (3'-HPT), a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells with IC50s of 9.0, 40.2, and 70.9 μM for COLO 205, HCT-116, and HT-29 cells, respectively, by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the p38MAPK , and PI3K Akt mTOR p70S6K pathways and activates the ERK1 2, JNK1 2 MAPK pathways[1].

GW 5074 (Raf1 Kinase Inhibitor I)(IC50=9 nM) is an effective and specific c-Raf inhibitor. It has no effect on the activities of JNK1 2 3, MEK1, MKK6 7, CDK1 2, c-Src, p38 MAP, VEGFR2 or c-Fms.

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.

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

CGP 57380 (MNK1 Inhibitor) is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases.

PT109 is a multikinase inhibitor that targets JNK and other kinases, playing a crucial role in anti-inflammatory, antioxidative, neurogenic, and synaptogenic processes. Specifically, PT109 inhibits JNK isoforms with the following IC50 values: JNK1 at 0.143 μM, JNK2 at 0.831 μM, and JNK3 at 0.285 μM. It also inhibits SGK isoforms (SGK1: IC50=1.34 μM; SGK2: IC50=5.6 μM; SGK3: IC50=26.4 μM) and ROCK2 (IC50=34 μM). Additionally, PT109 reprograms polymorphic glioblastoma multiforme (GBM) into oligodendroglia via the PTBP1 PKM1 2 pathway and alters the metabolic pattern of GBM to exhibit antiglioma activity.

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-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]

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

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

Potent and selective p38α and p38β degrader (DC50 < 50 nM). Displays no significant degradation of p38γ, p38δ, JNK1/2 or ERK1/2. Inhibits phosphorylation of MK2 in UV-treated cancer cells and LPS-stimulated bone marrow-derived macrophages (BMDM). Exhibits similar effect to p38α gene knockout in BBL358 cells. Active in vivo.

JNK-IN-18 (compound 23b) is a potent inhibitor of JNK1, boasting an IC50 of 2 nM. It demonstrates superior efficacy when compared to its IC50 values of 125 nM for JNK2 and 98 nM for BRAF(V600E).

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

MOMIPP is a PIKfyve inhibitor and a macropinocytosis inducer. MOMIPP readily penetrates the blood-brain barrier and is moderately effective in suppressing progression of intracerebral glioblastoma xenografts[1][2].