MAPK
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Catalog No.
Product Name
Application
Product Information
Product Citation
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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. -
p38 MAPK inhibitor
TAK 715 an inhibitor of p38 MAPK (IC50 = 7.1 nM for p38 MAPKα), Wnt/beta-catenin signaling, and Inhibits 22 kinases by more than 80%, including CK 1δ/ε. -
ERK1/ERK2 inhibitor
VRT752271 is a pyrrole inhibitors of ERK protein kinase.- Yuki Shimizu, .et al. , Cancer Lett, 2022, Sep 1;543 PMID: 35724767
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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 p38?? respectively). -
Raf kinase inhibitor
Sorafenib N-Oxide is a metabolite of Sorafenib, a potent Raf kinase inhibitor. -
ERK2 inhibitor
TCS ERK 11e (VX-11e) is a potent and selective extracellular signal-related kinase 2 (ERK2) inhibitor (Ki values are <2, 395, 540 and 852 nM for ERK2, GSK-3, Aurora Kinase A and Cdk2 respectively). Potently blocks proliferation of HT29 cells (IC50 = 48 nM). -
p38 MAPK inhibitor
Losmapimod, also know as GW856553 or GW856553X, is a drug developed by GlaxoSmithKline which acts as a selective inhibitor of the enzyme family known as p38 mitogen-activated protein kinases. -
RAF inhibitor
PF-04880594 is an inhibitor of RAF with IC50 values of 0.19 nM/0.13 nM and 0.39 nM for BRAF/BRAFV599E and c-RAF, respectively. -
JNK Inhibitor
JNK-IN-8 is the first irreversible JNK inhibitor for JNK1, JNK2 and JNK4 with IC50 of 4.7 nM, 18.7 nM and 1 nM, respectively- Mark P Roberto, .et al. , Immunity, 2021, Aug 10;54(8):1807-1824.e14 PMID: 34380064
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p38 MAPK inhibitor
Talmapimod (SCIO-469) is a selective, ATP-competitive p38 inhibitor (IC50 = 9 nM for p38α in vitro). -
ERK Inhibitor
SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 of 4 nM and 1 nM, respectively.- Yuki Shimizu, .et al. , Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- Yajun Li, .et al. , Cell Prolif, 2022, Oct;55(10) PMID: 35708050
- Sergey A. Dyshlovoy, .et al. , Pharmaceuticals, 2021, 14(10), 949
- Sergey A Dyshlovoy, .et al. , Sci Rep, 2020, Aug 6;10(1):13178 PMID: 32764580
- Guo X, .et al. , Pflugers Arch, 2018, Jun;470(6):909-921 PMID: 29441404
- Takuya Hasegawa, .et al. , FEBS Open Bio, 2017, Aug; 7(8): 1154-1165 PMID: 28781955
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MEK1/2 inhibitor
Refametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity. -
RAS/RAF/MAPK inhibitor
Diazepinomicin, also known as TLN-4601, is a small-molecule inhibitor of the RAS/RAF/MAPK signaling pathway with potential antineoplastic activity. -
Ras/Raf/MEK inhibitor
Balamapimod, also known as MKI-822, is a Ras/Raf/MEK inhibitor. -
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. -
Selective B-RAF Inhibitor
LGX818 is an orally available Raf kinase inhibitor with potential antineoplastic activity.- Seidel D, .et al. , Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
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pan-RAF inhibitor
TAK-632 is a potent pan-RAF inhibitor with favorable in vitro activity (BRAF(V600E) IC50, 2.4 nM; BRAF(wt), 8.3 nM; CRAF, 1.4 nM; pMEK (A375) IC50, 12 nM; pMEK (HMVII), 49 nM; V/B ratio.- Yosi Shamay, .et al. , Nat Mater, 2018, Apr; 17(4): 361-368 PMID: 29403054
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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. -
Raf/MEK dual inhibitor
RO5126766, also known as CH5126766, is a protein kinase inhibitor specific for the Raf and MEK mitogen-activated protein kinases (MAPKs) with potential anti-neoplastic activity.- Yuki Shimizu, .et al. , Cancer Lett, 2022, Sep 1;543 PMID: 35724767
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ERK5 inhibitor
XMD17-109 is a novel, specific inhibitor of ERK-5 with an EC50 value of 4.2 uM in HEK293 cells. -
ERK inhibitor
FR 180204 is a novel and selective inhibitor of extracellular signal-regulated kinase (ERK), which may be a potential new therapy for rheumatoid arthritis.- Sergey A Dyshlovoy, .et al. , Sci Rep, 2020, Aug 6;10(1):13178 PMID: 32764580
- Dyshlovoy SA, .et al. , Proteomics, 2017, Jun;17(11) PMID: 28445005
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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. -
MLK inhibitor
URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively.- Elad Prinz, .et al. , Mol Biol Cell, 2018, Oct 1; 29(20): 2470-2480 PMID: 30091641
