JNK-IN-13 (compound 1) is a potent and selective JNK inhibitor with IC50s of 290 nM and 500 nM for JNK3 and JNK2, respectively[1].
Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 µM) and GSK-3β (IC50=1.5 µM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research[1][2].
CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells[1]. CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways[2].
Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity[1].
AMG-548 is a potent, oral and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γand p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) [1]. AMG-548 inhibits Wnt signaling by direcly inhibing Casein kinase 1 isoforms δ and ε[2].
EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK[1][2].
NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
CHMFL-ABL-053 is a potent, selective and orally available Bcr-Abl/Src/p38 kinase inhibitor with IC50 of 70/62/90 nM; no inhibitory activity against c-Kit (>10 uM); inhibits the proliferation of CML cell lines K562 (GI50=14 nM), KU812 (GI50=25 nM), and MEG-01 (GI50=16 nM); completely suppresses tumor progression in the K562 cells inoculated xenograft mouse model with 50 mg/kg/day dosage treatment.
Dehydrocorydaline chloride is an alkaloidal that has anti-inflammatory and anti-cancer activities. Dehydrocorydaline chloride can elevate p38 MAPK activation.
DCZ19931 is a potent multi-targeting kinase inhibitor. DCZ19931 has anti-angiogenic effects on ocular neovascularization. DCZ19931 also inhibits ERK1/2-MAPK and p38-MAPK signaling[1].
LY-2584702 hydrochloride is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
Chloranthalactone B, a lindenane-type sesquiterpenoid, is a nature product that could be isolated from Chinese medicinal herb Sarcandra glabra. Chloranthalactone B inhibits the production of inflammatory mediators by inhibiting the AP-1 and p38 MAPK pathways[1].
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
SLV-2436 is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50s of 10.8 nM and 5.4 nM, respectively.
Methyllinderone is an inhibitor of AP-1/STAT/ERK. Methyllinderone has anti-inflammatory effect. Methyllinderone reduce the invasion and migration rate of TPA-stimulated MCF-7 cells. Methyllinderone can be used in study breast cancer metastasis[1].
B-Raf IN 6 (compound 2c) is a potent inhibitor of protein kinase B-Raf with an IC50 of 1.7 nM. B-Raf IN 6 is devoid of binding to the secondary target PXR and resists rapid metabolism. B-Raf IN 6 has the potential for the research of cancer disease[1].
Encorafenib (LGX818) is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
CI-1040 (PD184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
Laxiflorin B, a herbal compound, is a novel selective ERK1/2 inhibitor that has antitumor activity[1].
p38α inhibitor 1 is a p38α inhibitor extracted from patent WO 2008076265 A1.
TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM.IC50 value: 20 nMTarget: p38TA-02 is a novel compound with similar cardiogenic properties asSB203580 and SB202190. TA-02 especially inhibits TGFBR-2.
LUT014 is a B-Raf inhibitor with an IC50 of 11.7 nM, extracted from patent WO 2019026065A2 [1].
EVT801 is an orally active and selective inhibitor of VEGFR-3 (IC50=11 nM), which has antitumor effects. EVT801 inhibits not only VEGF-C-induced human endothelial cell proliferation, but also tumor (lymphatic) angiogenesis in tumor mouse models. EVT801 can reduce tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5) and myeloid derived suppressor cells (MDSC) production. EVT801 has synergistic effect with immune checkpoint therapy (ICT), which improves ICT response rate and has better inhibitory effect on cancer mouse models[1].
Diprovocim is a potent Toll-like receptor TLR1/TLR2 agonist that induces dose-dependent TNF production with EC50 of 110 pM in human THP-1 cells and 1.3 nM in primary mouse peritoneal macrophages; induces TNF production in bone marrow-derived dendritic cells (BMDC) with EC50 of 6.7 nM, also induces IL-6 production by mouse BMDC; induces phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα in THP-1 cells and mouse peritoneal macrophages, activates conventional TLR1/TLR2 signaling, including MAPK and canonical NF-κB signaling; synergizes with anti-PD-L1 to eliminate melanoma in mice.
Nedometinib is a tyrosine kinase inhibitor targeting to MEK1. Nedometinib has antineoplastic effect and can be used for research in dermatosis, cutaneous fibroneuroma, neurofibromatosis[1].
Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect[1].
TA-01 is a potent CK1 and p38 MAPK inhibitor, with IC50s of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively.
Lucidone, an anti-inflammatory agent that can be isolated from the fruit of Lindera erythrocarpa Makino. Lucidone inhibits LPS-induced NO and PGE2 production in RAW 264.7 mouse macrophages. Lucidone also decreases TNF-α secretion, iNOS and COX-2 expression. Lucidone prevents NF-κB translocation and inhibits JNK and p38MAPK signals. Lucidone also has inhibitory activity against Dengue virus (DENV) (EC50=25 μM)[1][2].
YL5084, a covalent JNK inhibitor, exhibits selectivity for JNK2 and JNK3 over JNK1 with IC50s of 70 nM, 84 nM and 2173 nM, respectively. YL5084 exhibits JNK2-independent antiproliferative effects and induces apoptosis in a JNK2-independent manner[1].