p38 Inhibitors: Small Molecules and Peptides
The p38 Mitogen-activated Protein Kinases (MAPKs) are a family of four related Ser/Thr kinases activated by proinflammatory cytokines and environmental stresses. All four p38 family members, alpha, beta, gamma, and delta, are phosphorylated by MKK3 and/or MKK6 at dual Thr and Tyr positions within the phosphoacceptor sequence Thr-Gly-Tyr. Once activated, p38 phosphorylates a number of targets, including the nuclear transcription factors ATF2 and Max.
The most frequently analyzed family member, p38 alpha, also known as SAPK2a and MAPK14, was initially purified as a kinase critical to the signaling cascade linking IL-1 to MAPKAPK-2 and the small heat shock protein HSP27. Ubiquitously expressed, p38 alpha is dually phosphorylated by MKK3 and MKK6 at Thr180 and Tyr182. Once activated, p38 alpha phosphorylates a number of targets, including the cytoplasmic kinases MNK 4 and PRAK5 and the nuclear transcription factors ATF2 1 and STAT1. Several promising compounds that inhibit p38 alpha are being investigated as potential therapies for arthritic and inflammatory diseases.
15 results for "p38 Inhibitors Small Molecules and Peptides" in Products
15 results for "p38 Inhibitors Small Molecules and Peptides" in Products
p38 Inhibitors: Small Molecules and Peptides
The p38 Mitogen-activated Protein Kinases (MAPKs) are a family of four related Ser/Thr kinases activated by proinflammatory cytokines and environmental stresses. All four p38 family members, alpha, beta, gamma, and delta, are phosphorylated by MKK3 and/or MKK6 at dual Thr and Tyr positions within the phosphoacceptor sequence Thr-Gly-Tyr. Once activated, p38 phosphorylates a number of targets, including the nuclear transcription factors ATF2 and Max.
The most frequently analyzed family member, p38 alpha, also known as SAPK2a and MAPK14, was initially purified as a kinase critical to the signaling cascade linking IL-1 to MAPKAPK-2 and the small heat shock protein HSP27. Ubiquitously expressed, p38 alpha is dually phosphorylated by MKK3 and MKK6 at Thr180 and Tyr182. Once activated, p38 alpha phosphorylates a number of targets, including the cytoplasmic kinases MNK 4 and PRAK5 and the nuclear transcription factors ATF2 1 and STAT1. Several promising compounds that inhibit p38 alpha are being investigated as potential therapies for arthritic and inflammatory diseases.
Potent, selective inhibitor of p38 MAPK
| Chemical Name: | 4-[4-(4-Fluorophenyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]phenol |
| Purity: | ≥99% (HPLC) |
Selective inhibitor of p38 MAPK
| Chemical Name: | 4-[5-(4-Fluorophenyl)-2-[4-(methylsulfonyl)phenyl]-1H-imidazol-4-yl]pyridine |
| Purity: | ≥98% (HPLC) |
High affinity and selective p38 kinase inhibitor
| Alternate Names: | Doramapimod |
| Chemical Name: | N-[3-(1,1-Dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-N'-[4-[2-(4-morpholinyl)ethoxy]-1-naphthalenyl]urea |
| Purity: | ≥98% (HPLC) |
Selective inhibitor of p38 MAPK; water-soluble
| Chemical Name: | 4-[5-(4-Fluorophenyl)-2-[4-(methylsulphonyl)phenyl]-1H-imidazol-4-yl]pyridine hydrochloride |
| Purity: | ≥98% (HPLC) |
Potent, selective p38 MAPK inhibitor; orally active
| Chemical Name: | trans-4-[4-(4-Fluorophenyl)-5-(2-methoxy-4-pyrimidinyl)-1H-imidazol-1-yl]cyclohexanol |
| Purity: | ≥98% (HPLC) |
Selective inhibitor of p38α-mediated MK2a phosphorylation; also tubulin polymerization inhibitor
| Chemical Name: | 2'-Fluoro-N-(4-hydroxyphenyl)-[1,1'-biphenyl]-4-butanamide |
| Purity: | ≥99% (HPLC) |
Selective inhibitor of p38α and p38β2
| Chemical Name: | (2-Methylphenyl)-[4-[(2-amino-4-bromophenyl)amino]-2-chlorophenyl]methanone |
| Purity: | ≥98% (HPLC) |
Potent, selective p38α and p38β inhibitor
| Chemical Name: | 4-[4-(4-Fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-3-butyn-1-ol |
| Purity: | ≥98% (HPLC) |
Potent and selective p38α inhibitor
| Alternate Names: | VX745,VX-745,Neflamapimod |
| Chemical Name: | 5-(2,6-Dichlorophenyl)-2-[2,4-difluorophenyl)thio]-6H-pyrimido[1,6-b]pyridazin-6-one |
| Purity: | ≥98% (HPLC) |
Potent p38 MAPK inhibitor; anti-inflammatory
| Chemical Name: | N-[4-[2-Ethyl-4-(3-methylphenyl)-5-thiazolyl]-2-pyridinyl]benzamide |
| Purity: | ≥99% (HPLC) |
p38 MAPK inhibitor; anti-inflammatory
| Chemical Name: | N-Cyclopropyl-4-[4-(4-fluorophenyl)-2-(4-piperidinyl)-5-thiazolyl]-2-pyrimidinamine dihydrochloride |
| Purity: | ≥98% (HPLC) |
Potent and selective p38α/β inhibitor
| Chemical Name: | (-)-3-[3-Bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxo-1(2H)-pyridinyl]-N,4-dimethylbenzamide |
| Purity: | ≥98% (HPLC) |
Potent and selective p38α inhibitor
| Chemical Name: | 2-[[(2S)-2-Amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone |
| Purity: | ≥98% (HPLC) |
Selective p38 MAPK inhibitor
| Chemical Name: | 6-Chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-α-oxo-1H-Indole-3-acetamide hydrochloride |
| Purity: | ≥98% (HPLC) |
p38 MAPK inhibitor
| Chemical Name: | N-Cyano-N'-[2-[[8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)-7,8-dihydro-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]ethyl]guanidine |
| Purity: | ≥98% (HPLC) |
