MAPK Signaling

Azosemide, a sulfonamide loop diuretic, is a potent NKCC1 inhibitor with IC50s of 0.246??M and 0.197??M for hNKCC1A and NKCC1B, respectively.

CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.

GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM).

JWG-071 is the first reported kinase-selective chemical probe for ERK5. JWG-071 improves ERK5 activity and BRD4 selectivity. JWG-071 will be a much-needed chemical probe for deconvoluting ERK5 and BRD4 pharmacology.

A flavonoid with diverse biological activities

Tenuifoliside A is isolated from Polygala tenuifolia, has anti-apoptotic and antidepressant-like effects.

Isoliquiritin apioside significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis of cancer cells and endothelial cells.

2,5-Dihydroxyacetophenone, isolated from Rehmanniae Radix Preparata, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways.

A dual inhibitor of CK2 and ERK8

A dual inhibitor of p38α and p38β MAPKs

M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.

Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6.

CCT241161 is a multi-kinase inhibitor that inhibits B-RAF, B-RAFV600E, C-RAF, Src, and LCK (IC50s = 252, 15, 6, 15, and 3 nM, respectively).

Regorafenib-13C-d3 is intended for use as an internal standard for the quantification of regorafenib by GC- or LC-MS.

Milrinone-d3 is intended for use as an internal standard for the quantification of milrinone by GC- or LC-MS.

Cafestol, one of the major components of coffee, is a coffee-specific diterpene form and an inhibitor of ERK2.

Ferulic acid is a hydroxycinnamic acid that is abundant in plants and originally derived from giant fennel (F.

CAY10706 is a ligustrazine-curcumin hybrid that promotes intracellular reactive oxygen species accumulation preferentially in lung cancer cells.

Inflachromene is an inhibitor of HMGB1 and HMGB expression. Inflachromene can inhibit the release of HMGB1 and the NF-κB signaling pathway, exerting anti-inflammatory and neuroprotective effects. Inflachromene is mainly used to treat epilepsy.

5-trans PGE2 occurs naturally in some gorgonian corals and is a common impurity in commercial lots of PGE1.

Nε-(1-Carboxymethyl)-L-lysine is a unique post-translational modification (PTM) of proteins that is generated by the non-enzymatic glycation of lysine residues.

Theaflavin 3,3'-digallate (TF-3; ZP10) is a potent inhibitor of Zika virus (ZIKV) protease with an IC 50 value of 2.3μM.

Phosphodiesterase 4 (PDE4) inhibitor is an inhibitor of PDE4 with an IC50 value of 0.10 μM for the human recombinant enzyme.

2-Arachidonoyl glycerol (2-AG) is an endogenous central cannabinoid (CB1) receptor agonist that is present at relatively high levels in the central nervous system.