jnk-3 inhibitor-1

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.

SKLB-163 is a small-molecule inhibitor and a RhoGDI inhibitor with oral bioactivity, cell permeability, and selectivity. This compound induces tumor cell apoptosis, inhibits proliferation and migration, and enhances radiosensitivity by downregulating RhoGDI, activating the JNK-1/caspase-3 pathway, and suppressing Akt and p44/42 MAPK phosphorylation.

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.

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.

JNK-1-IN-4 (Compound E1) is an inhibitor of JNK, targeting JNK-1, JNK-2, and JNK-3 with IC50 values of 2.7, 19.0, and 9.0 nM, respectively. This compound inhibits the phosphorylation of c-Jun and reduces the expression of TGF-β1-induced EMT markers (such as fibronectin and α-SMA). JNK-1-IN-4 exhibits favorable pharmacokinetic properties with a bioavailability of 69%. Additionally, it demonstrates antifibrotic effects in a Bleomycin-induced mouse model of idiopathic pulmonary fibrosis.

Ro 31-8220 formic is a potent inhibitor of protein kinase C (PKC), specifically targeting PKCα, PKCβI, PKCβII, PKCγ, PKCε, and rat brain PKC, with IC50 values of 5, 24, 14, 27, 24, and 23 nM, respectively. It also inhibits MAPKAP-K1b, MSK1, S6K1, and GSK3β, with IC50 values of 3, 8, 15, and 38 nM. Additionally, Ro 31-8220 formic suppresses the expression of MKP-1, induces c-Jun expression, and activates JNK, exhibiting these effects through mechanisms independent of PKC.

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

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]