CC-401 hydrochloride is a second generation ATP-competitive anthrapyrazolone c-Jun N terminal kinase (JNK) inhibitor with potential antineoplastic activity.
CEP-32496 hydrochloride is a highly potent inhibitor of wild-type BRAF, V600E mutant BRAF and c-Raf with Kd values of 14 nM, 36 nM and 39 nM, respectively.
Cobimetinib R-enantiomer is the R-enantiomer of Cobimetinib, which is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase(MEK1/2).
Dabrafenib Mesylate is a novel, potent, and selective Raf kinase inhibitor that is capableof inhibiting the kinase activity of wild-type B-Raf, B-RafV600Eand c-Raf with IC50 values of 3.2, 0.8, and 5.0 nM, respectively.
NG25, a TAK1 inhibitor, inhibited the activation of IKK by TLR7 and TLR9 agonists and prevented the secretion of type 1 IFNs induced by these ligands in Gen2.2 cells.
Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
Cercosporamide, an usnic amide, was originally identified in Cercosporidium henningsii as a host-selective phytotoxin and broad-spectrum antifungal agent and is a potent inhibitor of MAP-kinase interacting kinase-2 (Mnk2; IC50 = 11 nM), JAK3 (IC50 = 31), and Mnk1 (IC50 = 116 nM).
BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
DEL-22379 is a potent and selective ERK Dimerization inhibitor that inhibits ERK Dimerization without affecting ERK phosphorylation, forestalls tumorigenesis driven by RAS-ERK pathway oncogenes.
PLX7904 is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells.
AL-8697 is a selective p38 MAPK(mitogen-activated protein Kinase) inhibitor, which is also named P38α inhibitor. It has the function of inhibiting the activity of P38 MAPK.
OTS514, a thieno[2,3-c]quinolone compound, is a highly potent TOPK inhibitor with an IC50 value of 2.6 nM. The compound can inhibit TOPK kinase activity.
IQ 3 is a selective JNK3 inhibitor (Kd values are 66, 240 and 290 nM for JNK3, JNK1 and JNK2 respectively). Inhibits NF-kB/AP1 transcriptional activity in THP1-Blue cells (IC50 = 1.4 μM). Also inhibits TNF-α and IL-6 production in vitro.
SU 3327 is a selective inhibitor of JNK (c-Jun N-terminal kinase)(IC50 = 0.7uM). SU 3327 is shown to inhibit the protein-protein interaction between JNK and JIP (IC50 = 239 nM).
CMPD-1 is a non-ATP-competitive, selective inhibitor of p38α-mediated MK2a (mitogen-activated protein kinase-2a) phosphorylation (apparent Ki = 330 nM).
JIP-1 (153-163) is a peptide inhibitor of c-Jun N-terminal kinase (JNK), based on residues 153-163 of JNK-interacting protein-1 (JIP-1). Binds to JNK with affinity in the micromolar range and minimally inhibits p38 and ERK.
HI-TOPK-032 is a potent and selective TOPK inhibitor. In vitro, HI-TOPK-032 strongly suppressed TOPK kinase activity but had little effect on extracellular signal-regulated kinase 1 (ERK1), c-jun-NH2-kinase 1, or p38 kinase activities.
SB 706504 is a p38 MAPK inhibitor, preventing LPS-induced transcription of a range of chemokineis and cytokines in chronic obstructive pulmonary disease monocyte derived macrophages.
ERK5-IN-1 exhibits potent inhibition of ERK5 with cellular EC50 values of 0.19 uM and enzymatic IC50 values of 0.087 uM and of LRRK2[G2019S] with enzymatic IC50 values of 0.026uM.
PNRI-299 is a selective AP-1 transcription inhibitor with IC50 of 20 uM without affecting NF-kappaB transcription (up to 200 μM) or thioredoxin (up to 200 μM).
MK-8353 (SCH900353) is an orally bioavailable, selective, and potent ERK inhibitor that inhibits activated ERK1 and ERK2 in vitro, with IC50 values of 23.0 nM and 8.8 nM, respectively (IMAP kinase assay), and nonactivated ERK2, with an IC50 of 0.5 nM (MEK1-ERK2-coupled assay).
PLX8394 is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity.
LXH254 is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays.