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You are here:Home-Inhibitors & Agonists-Ras-Raf-MAPK-ERK Pathway-p38 MAPK

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The p38 MAPK family consists of highly conserved proline-directed serine-threonine protein kinases that are activated in response to a number many growth factors, cytokines, and chemotactic substances, such as vascular endothelial growth factor (VEGF), fibroblast growth factor (FGF), PDGF, TNF, interleukins, lipopolysaccharide (LPS) and formyl-methionyl-leucyl-phenylalanine (fMLP). It is well known that p38 is involved in inflammation, apoptosis, cardiomyocyte hypertrophy and cell differentiation.

The p38 MAPK family is composed of four proteins: p38α (encoded by the gene Mapk14), p38β (Mapk11), p38γ (Mapk12), and p38δ (Mapk13). Their coding genes have a distinct tissue distribution and they appear differentially expressed, being Mapk14 the most highly expressed. p38 MAPKs are substrates for three MAP2K (MKK6, MKK3, and MKK4). The contribution of each of these MAP2K to p38 MAPKs activation depends on the stimulus and the cell type. The MAP3Ks that lead to p38 MAPKs activation are ASK1, DLK1, TAK1, TAO1, TAO2, TPL2, MLK3, MEKK3, MEKK4, and ZAK1.

Cat. No. Product Name CAS No. Information
H9553

Emprumapimod

 		765914-60-1

Emprumapimod is a potent, orally bioavailable and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain.
H7455

VX-745

 		209410-46-8

A potent and selective p38α kinase inhibitor with IC50 of 9 nM; shows 20-fold selectivity for p38α over p38β (Ki=220 nM) and no significant inhibition for MAP kinases (with the exception of MKK6); exhibits inhibition of PBMC IL-1β and TNFα IC50 of 45 and 51 nM, respectively; possesses favorable PK profile, and demonstrates good in vivo activity in models of inflammation.
H7454

VX-702

 		745833-23-2

A potent, selective, second generation p38 MAPK inhibitor with IC50 of 4-20 nM for p38α; displays 14-fold higher potency against the p38α versus p38β; inhibits p38 activation induced by platelet agonists including thrombin, SFLLRN, AYPGKF, U46619 and collagen, without effect on collagen-mediated platelet aggregation.
H7453

TAK-715

 		303162-79-0

A potent, selective, orally active p38α MAPK inhibitor with IC50 of 7.1 nM; displays >20-fold selectvity over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1; inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM; exerts significant efficacy in rat adjuvant-induced arthritis model.
H7452

TA-02

 		1784751-19-4

A potent p38 MAPK inhibitor with IC50 of 20 nM; inhibits the phosphorylation of proteins downstream of p38α MAPK such as MAPKAPK2 and HSP27 during cardiogenesis, and increases ATF-2 and MEF2C during cardiac differentiation.
H7451

SKF-86002

 		72873-74-6

SKF-86002 is a potent inhibitor of p38 MAPK with IC50 of 0.5-1 uM, inhibits LPS-induced IL-1 and TNF-α production in human monocyte with IC50 of 1 uM; inhibits prostaglandin H2 (PGH2) synthase activity (IC50=120 uM) as well as prostanoid production by rat basophilic leukemia (RBL-1) cells (IC50=70 uM); blocks superoxide anion production in response to FMLP and reduces adhesion and chemotaxis in response to PAF or FMLP in human neutrophils; also inhibits 5-lipoxygenase- and cyclooxygenase-mediated arachidonic acid metabolism in RBL-1 cells (IC50=10 and 100 uM respectively), shows anti-inflammatory in vivo.
H7450

SD 0006

 		271576-80-8

SD-06 is a p38 MAP kinase inhibitor, inhibits p38α with IC50 of 170 nM and inhibits LPS-stimulated TNF-release in rats ((83% inhibition at 1mg/kg, po).
H7449

SCIO-469

 		309913-83-5

A potent, selective p38α MAPK inhibitor with IC50 of 9 nM; displays 10-fold selectivity for p38α over p38β, >2,000-fold selectivity over a panel of 20 other kinases, including other MAP kinases; decreases apoptosis in MDS CD34+ progenitors and leads to dose-dependant increases in erythroid and myeloid colony formation; enhances the ability of MG132 and bortezomib to induce the apoptosis of MM cells, and inhibits tumor growth in vivo.
H7448

SC-806

 		216505-89-4

A potent, orally active p38 MAPK inhibitor with IC50 of 50 nM, significantly decreases incidence of arthritis in mouse collagen-induced arthritis.
H7447

SB-242235

 		193746-75-7

A selective p38 MAPK inhibitor; inhibits IL-1 beta induction of p38 MAPK in primary human chondrocytes with IC50 of 1 uM; inhibits LPS-stimulated serum levels of TNFalpha in normal rats with mean ED50 of 3.99 mg/kg.

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