MAPK
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Catalog No.
Product Name
Application
Product Information
Citations
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pan RAF inhibitor
Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. -
Raf inhibitor
ML 786 dihydrochloride is a potent Raf kinase inhibitor (IC50 values are 2.1, 2.5 and 4.2 nM for B-RafV600E, C-Raf and wild-type B-Raf respectively). -
pan-Raf inhibitor
MLN 2480 is an oral, selective pan-Raf kinase inhibitor in chinical trials. -
MEK inhibitor
Refametinib is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively. -
MK2 Inhibitor
PF-3644022 is a potent and selective mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK2) inhibitor (Ki =3 nM). -
VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor
Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively. -
p38 MAPK inhibitor
SB 239063 is a potent and selective p38 MAP kinase inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580. SB 239063 reduces inflammatory cytokine production and is neuroprotective following oral administration in vivo. -
JNK Inhibitor IX
TCS JNK 5a is a highly selective inhibitor of JNK2 and JNK3 (pIC50 values are 6.7, 6.5, <5.0 and <4.8 for JNK3, JNK2, JNK1 and p38α respectively).
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Raf kinase inhibitor
Sorafenib N-Oxide is a metabolite of Sorafenib, a potent Raf kinase inhibitor. -
ERK1/2 inhibitor
GDC-0994 is a potent and selective Erk1/2 inhibitor. GDC-0994 inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways. -
p38 MAPK inhibitor
Pamapimod is a novel p38 mitogen-activated protein kinase inhibitor. -
p38 MAPK inhibitor
BMS-582949 Is a Dual Action p38 Kinase Inhibitor Well Suited To Avoid Resistance Mechanisms That Increase p38 Activation in Cells. -
JNK inhibitor
CC-930 is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ?? 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ?? 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively -
MAPKAP-K2 (MK-2) inhibitor
MK-2 Inhibitor III (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM. -
ERK5 inhibitor
XMD17-109 is a novel, specific inhibitor of ERK-5 with an EC50 value of 4.2 uM in HEK293 cells. -
B-Raf inhibitor
B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively -
MKK/MEK inhibitor
SL-327 is a selective inhibitor of MEK1 and MEK2 (IC50 values are 0.18 and 0.22 μM respectively); blocks hippocampal LTP in vitro. Brain penetrant in vivo, blocking fear conditioning and learning in rats, and producing neuroprotection in mice, following systemic administration. -
TOPK inhibitor
OTS964 is a potent TOPK inhibitor with an IC50 value of 28 nM. -
PARP-1 inhibitor
TAK1/MAP4K2 inhibitor 1 is a potent dual inhibitor targeting transforming growth factor β-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), exhibiting IC₅₀ values of 41.1 nM and 18.2 nM, respectively.
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dual BRAF inhibitor
AZ304 is a potent dual BRAF inhibitor targeting the kinase domains of wild type BRAF, V600E mutant BRAF. AZ304 exerted potent inhibitory effects on both wild type and V600E mutant forms of the serine/threonine-protein kinase BRAF, with IC50 values of 79?nM and 38?nM, respectively. -
MEK1 inhibitor
Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM. -
MAP4K4 inhibitor
PF-06260933 is a potent, selective, orally available MAP4K4 inhibitor with IC50 of 3.7 nM.
