JNK Inhibitor

JNK-1-IN-4 (Compound E1) is an inhibitor for JNK, that inhibits JNK-1, JNK-2 and JNK-3 with IC₅₀s of 2.7, 19.0 and 9.0 nM, respectively. JNK-1-IN-4 inhibits the phosphorylation of c-Jun, and reduces the expression of TGF-β1-induced EMT marker proteins, such as fibronectin and α-SMA. JNK-1-IN-4 exhibits good pharmacokinetic characteristics with a bioavailability of 69%. JNK-1-IN-4 exhibits anti-fibrotic effect in Bleomycin (HY-17565)-induced mice idiopathic pulmonary fibrosis models.

Trimebutine-d₃ hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

Emodic acid (NSC624610) is an anthraquinone compound isolated from A. microcarpus, which can inhibit the proliferation of cancer cells by inhibiting the activity of NF-κB. Emodic acid can also inhibit the phosphorylation of p38, ERK and JNK, the secretion of tumor-promoting cytokines IL-1β and IL-6, and the expression of VEGF and MMP, thereby inhibiting the invasion and migration potential of cancer cells.

ASK1-IN-12 is an ASK1 inhibitor with an IC₅₀ of 6.3 nM. ASK1-IN-12 inhibits TNF-α-induced activation of the ASK1-p38/JNK pathway. ASK1-IN-12 can reduce free fatty acid-induced cholesterol increase, lipid droplet accumulation and improves hepatocellular steatosis. ASK1-IN-12 can be used for the research of non-alcoholic steatohepatitis (NASH).

Akt/NF-κB/MAPK-IN-1 (compound 2m) is a potent and orally active inhibitor against NO (IC₅₀=7.70 μM) with no significant toxicity. Akt/NF-κB/MAPK-IN-1 shows anti-inflammatory activity by inhibiting Akt/NF-κB and MAPK signaling pathways.

RANKL-IN-1 formate is a selective receptor activator of nuclear factor-κB ligand inhibitor ligand (RANKL) inhibitor with a K_D value of 7.6 μM. RANKL-IN-1 formate exhibits inhibitory activity and selectivity against osteoclastogenesis with an IC₅₀ value of 0.07 μM and SI of 82.57. RANKL-IN-1 formate binds directly to RANKL and blocks the RANKL-induced activation of the NF-κB and MAPK pathways. RANKL-IN-1 formate can be used for the research of metabolic disease, such as osteoporosis.

Pipoxolan hydrochloride is an anti-spasmotic agent. Pipoxolan hydrochloride induces Apoptosis, increases intracellular ROS. Pipoxolan hydrochloride down-regulates phosphorylation JNK and p38, and then, MMP-2 and -9. Pipoxolan hydrochloride relieves smooth muscle spasms in the digestive, urinary, and gynecological systems. Pipoxolan hydrochloride also exhibits anticancer activity against leukemia, oral squamous cell carcinoma, and lung adenocarcinoma.

Mapk9 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Mapk9 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Pulegone-d₈ is deuterated labeled Pulegone (HY-N1500). Pulegone is a monoterpene ketone compound widely present in the essential oils of many plants. Pulegone can also be used as a bird repellent. Pulegone has multiple activities such as anti-inflammatory, antibacterial, antifungal, and anti-hyperalgesic effects. Pulegone is particularly effective against bacteria of the Salmonella species.

CLP-d2 is a multi-target anti-inflammatory agent, osteoclastogenesis inhibitor and immunomodulator with superior pharmacokinetic properties to Daptomycin (HY-B0108) and good safety profiles. CLP-d2 inhibits the NF-κB and MAPK signaling pathways by reducing the expression levels of c-Fos and NFATc1, and decreasing the phosphorylation levels of IκBα, p65, ERK and JNK, thereby reducing the secretion of pro-inflammatory cytokines such as IL-6, TNF-α and IL-1β to exert anti-inflammatory activity. CLP-d2 inhibits intra-articular osteoclastogenesis in mice, alleviates bone erosion and joint swelling, reduces synovial hyperplasia and inflammatory cell infiltration, and decreases serum rheumatoid factor (RF) levels. CLP-d2 is applicable to related research on rheumatoid arthritis.

TOPK-p38/JNK-IN-1 (Compound B12) is an orally active TOPK-p38/JNK signaling pathway inhibitor with the IC₅₀ value of 2.14 µM for NO production. TOPK-p38/JNK-IN-1 shows anti-inflammatory activities. TOPK-p38/JNK-IN-1 also inhibits phosphorylate downstream related proteins and avoids degradation of TOPK.

Catenarin, an anthraquinone compound, inhibits CCR5- and CXCR4-mediated chemotaxis. Catenarin reduces the phosphorylation of mitogen-activated protein kinases (p38 and JNK) and their upstream kinases (MKK6 and MKK7), and calcium mobilization. Catenarin shows anti-inflammatory effect and suppresses leukocyte migration in the diabetes. Catenarin exhibits significant inhibitory effects against Gram-positive bacteria. Catenarin prevents type 1 diabetes (T1D) in nonobese diabetic mice^[1][2].

ZG-10 (JNK-IN-2) is a JNK inhibitor, with IC₅₀ values of 809 nM, 1140 nM and 709 nM for JNK1, JNK2, and JNK3, respectively. ZG-10 (JNK-IN-2) is a potential anti-SARS-CoV-2 agent.

JNK3 inhibitor-9 (Compound 24a) is a potent, selective and BBB-permeable JNK3 inhibitor with an IC₅₀ value of 12 nM. JNK3 inhibitor-9 also potently inhibits GSK3α/β (IC₅₀s: 14 and 35 nM, respectively) involved in Tau phosphorylation. JNK3 inhibitor-9 reduces c-Jun and APP phosphorylation. JNK3 inhibitor-9 protects neurons from Aβ_1-42 toxicity.

Trimebutine-d₅ fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

α-Neoendorphin porcine is a peptide. α-Neoendorphin porcine effectively alleviates UVB-induced skin photoaging via activating mTOR-Beclin-1-mediated autophagy, reducing UVB-triggered ROS production, inhibiting the MAPK pathway and MMP activity, and promoting type I procollagen synthesis. α-Neoendorphin porcine exerts anti-aging and anti-wrinkle effects on skin cells. α-Neoendorphin porcine can be used in studies related to skin photoaging.

JIP-1(153-163) TFA (TI-JIP TFA) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide).

Iso-AS601245 TFA is an orally active JNK inhibitor, with IC₅₀ values of 0.15 μM, 0.22 μM and 0.07 μM against JNK1, JNK2 and JNK3, respectively. Iso-AS601245 TFA reduces plasma TNF-α levels in mice and inhibits IL-2 secretion in activated T cells. Iso-AS601245 TFA alleviates adjuvant-induced rheumatoid arthritis in mice. Iso-AS601245 TFA can be used in studies related to rheumatoid arthritis.

SR-3737 is a JNK3 and p38 inhibitor (IC₅₀: 12 and 3 nM).

Cyy-272 is an orally active JNK inhibitor with IC₅₀ values of 1.25 μM for JNK1, 1.07 μM for JNK2, and 1.24 μM for JNK3. Cyy-272 exerts anti-inflammatory effects by inhibiting JNK phosphorylation, thereby alleviating acute lung injury (ALI) induced by lipopolysaccharide (LPS, HY-D1056). Additionally, Cyy-272 significantly reduces inflammation in cardiomyocytes and cardiac tissue induced by high lipid concentrations, further mitigating cardiac hypertrophy, fibrosis, and apoptosis. Cyy-272 can be used in the study of obese cardiomyopathy.