α-mapi

MAPI is an irreversible peptidyl 3C cysteine protease (SV3CP) inhibitor. By covalently attaching its C-terminal Michael acceptor moiety to the active site thiol of SV3CP Cys 139, MAPI inhibits SV3CP. It shows potential for use in the study of norovirus infections.

Adezmapimod (SB 203580) is a selective, ATP-competitive p38 MAPK inhibitor (IC50=0.3-0.5 μM) that activates autophagy and mitochondrial autophagy, with more than 100-fold higher selectivity over PKB, LCK, and GSK-3β.

Doramapimod (BIRB 796) is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70.

Talmapimod (SCIO-469) is a selective, orally active, ATP-competitive p38α inhibitor with IC50 values of 9 nM for p38α and 90 nM for p38β. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs.

Emprumapimod (PF-07265803) is an orally active and specific inhibitor of mitogen-activated protein kinase p38α MAPK, inhibits LPS-induced production of IL-6, and can be used to study dilated cardiomyopathy induced by the LMNA gene.

Azacyclonol (MER 17) is a drug used to diminish hallucinations in psychotic individuals.

Dilmapimod (SB-681323) is a potent inhibitor of p38 MAPK, potentially suppressing inflammation in chronic obstructive pulmonary disease.

Talmapimod hydrochloride is a selective and ATP-competitive p38α inhibitor (IC50: 9 nM). It also shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.

Balamapimod, also known as MKI-822, is a small-molecule Ras/Raf/MEK inhibitor that directly targets deregulated MAPK signaling cascades and is being actively explored to suppress aberrant protein kinase activity implicated in oncogenic transformation, inflammatory signaling, and pathological cell proliferation, with demonstrated therapeutic relevance for stroke, osteoporosis, rheumatoid arthritis, polycystic kidney disease, colonic polyps, and other inflammation-driven disorders through pathway-level inhibition.

Timapiprant sodium inhibits mast cell activation of Th2 lymphocytes and eosinophils. Timapiprant sodium is a potent and selective D prostanoid receptor 2 antagonist. Timapiprant sodium potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), ra

Losmapimod hydrochloride (GW856553X) is an orally active, potent, and highly selective p38 alpha/beta MAPK inhibitor (IC50 = 0.8 nM). It greatly reduces the release of pro-inflammatory cytokines, including TNF-alpha and IL-6, by blocking inflammatory signaling cascades, showing remarkable efficacy in COPD and severe cardiovascular inflammation models.

SB 203580 hydrochloride (Adezmapimod hydrochloride) is a selective, ATP-competitive p38 MAPK inhibitor that induces mitochondrial autophagy and cytosolic autophagy and inhibits SAPK2a/p38, SAPK2b/p38β2, LCK, GSK3β, and PKBα. SB 203580 hydrochloride has been shown to be useful in antiretroviral therapy. 203580 hydrochloride inhibits amphoteric mechanical anomalous pain in a mouse model of antiretroviral-induced neuropathic pain.

Losmapimod (GSK-AHAB) (GW856553X; SB856553; GSK-AHAB) is a specific, potent, and orally active p38 MAPK inhibitor (pKi: 8.1/7.6 for p38α/β).

Timapiprant (OC000459) is a potent and selective D prostanoid receptor 2 (DP2) antagonist (IC50: 13 nM).

Bentamapimod (AS 602801) is a novel, orally active inhibitor of JNK.

Relmapirazin may be used as a diagnostic agent.

Semapimod hydrochloride dihydrate is a biochemical.

Semapimod mesylate is a biochemical.

Telmapitant is an antagonist of the neurokinin NK1 receptor.

Semapimod tetrahydrochloride (CPSI-2364 tetrahydrochloride) is a synthetic ornithine mitogen-activated protein kinase blocker and pro-inflammatory cytokine production inhibitor that interferes with macrophage and microglia function. Sematimod tetrahydrochloride inhibits TLR4 signaling, TNF-α, IL-1β, and IL-6, and is used in the study of Crohn's disease and other inflammatory conditions.

Suc-Ile-Glu(γ-pip)-Gly-Arg-pNA hydrochloride is a chromogenic substrate specifically designed for factor Xa.

Rehmapicroside is a natural product of Rehmannia, Scrophulariaceae. The catalog number is T3S0462 and the CAS number is 104056-82-8. Rehmapicroside can be used as a reference standard.

Neflamapimod (VX-745) , a specific and effective inhibitor of p38α(IC50=10 nM), is 22-fold greater specificity against p38β and no inhibition activity to p38γ.

Dilmapimod tosylate is a potent p38 mitogen-activated protein kinase (MAPK) inhibitor. It was investigated for its anti-inflammatory effect in non-head injury trauma patients at risk for developing acute respiratory distress syndrome. IL-1β was identified as a gene regulated by dilmapimod that could influence c-reactive protein levels. Dilmapimod had been in phase III clinical trials by GlaxoSmithKline for the treatment of rheumatoid arthritis, neuropathic pain, coronary artery disease (CAD) and chronic obstructive pulmonary disease (COPD).