MAPK
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Catalog No.
Product Name
Application
Product Information
Product Citation
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MEK1 inhibitor
Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases.- Yunping Hu, .et al. , Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
- Seidel D, .et al. , Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
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MEK1/2 inhibitor
MEK162 (ARRY-438162) is a potent, selective, ATP uncompetitive inhibitor of MEK1/2.- S Shahab, .et al. , J Neuropathol Exp Neurol, 2020, Jul 1;79(7):746-753
- Seidel D, .et al. , Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
- Alquezar C, .et al. , Eur Neuropsychopharmacol, 2015, Mar;25(3):386-403 PMID: 25624003
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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. -
nAChR agonist
Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does. -
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. - Asiaticoside (Madecassol) is the active chemical component of the plant Centella asiatica. Asiaticoside is used to study potential treatments for wounds and burns.
- trans-Zeatin is a member of the plant hormone family known as ??cytokinins??, which regulate cell division, development, and nutrient processing.
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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. -
food flavouring
2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) is a mixture of dihydroxyacetophenone isomers is used in food flavouring. 2',5'-Dihydroxyacetophenone significantly inhibits NO production via the suppression of iNOS expression. 2',5'-Dihydroxyacetophenone significantly decreases levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways. -
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. - Hypothemycin is a resorcylic acid lactone polyketide. It was found to inhibit the proliferation of mouse and human T cells stimulated with anti-CD3 mAb + PMA and of human PBMC stimulated with anti-CD3 mAb alone.