p42

Zibotentan (ZD4054) (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.

NTP42 is an antagonist of thromboxane A2 (TXA2) receptor(IC50 of 3.278 nM)

SP4206 is an interaction inhibitor of IL-2 IL-2Rα (IL-2 and IL-2Rα with Kd of 70 nM and 10 nM,respectively)

AMP423 is a naphthyl derivative of 2-cyanoaziridine-1-carboxamide with structural similarity to the pro-oxidant anti-tumor agent imexon. AMP423 was active in SCID mice bearing 8226 S myeloma and SU-DHL-6 B-cell lymphoma tumors, with a median tumor growth delay (T-C) of 21 days (P = 0.0002) and 5 days (P = 0.004), respectively, and a median tumor growth inhibition (T C) of 33.3% (P = 0.03) and 82% (P = 0.01), respectively. In non-tumor-bearing mice, AMP423 was not myelosuppressive.

Enniatins B decreases the activation of ERK (p44 p42). Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using rat liver microsomes.

Enniatin B1, a Fusarium mycotoxin, crosses the blood-brain barrier, decreases the activation of ERK (p44 p42), and inhibits moderately TNF-α-induced NF-κB activation. Furthermore, it inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity, exhibiting an IC50 of 73 μM in rat liver microsome enzyme assays.

CYM5442 is an S1P agonist, targeting to Sphingosine.

Albofungin is a xanthone isolated from A. tumemacerans.

STO-609 acetate is selective, cell-permeable inhibitor of Ca2+-calmodulin-dependent protein kinase kinase (Ki: 80/15 ng/ml, for CaM-KKα/KKβ); competes for the ATP-binding site. It displays > 80-fold selectivity over CaMK1/2/4, PKC, MLCK, PKA and p42 MAPK.

AG126 (Tyrphostin AG126) selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM. It blocks the production of TNF-α in vitro2 and in vivo, attenuating signaling through NF-κB, the induced expression of COX-2 and iNOS, and the inflammatory response in diverse animal models. AG-126 weakly inhibits epidermal GFRK (IC50: 450 μM) and platelet-derived GFRK (IC50 > 100 μM).

CYM 5442 hydrochloride is a potent and selective S1P1agonistin vitro(EC50 = 1.35 nM). Activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1. Induces acute lymphopenia in mice. Brain penetrant.

Olodanrigan (EMA401), a highly selective AT2R antagonist, inhibition of augmented AngII AT2R induced p38 and p42 p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons. EMA401 blocks p38, p42 p44 mitogen-activated protein kinase (MAPK) activation, neurite outgrowth in adult rat DRG neurons, and sensitization of adult rat and human DRG neurons induced by AngII. It inhibits capsaicin responses in cultured hDRG neurons.

Ki16425 (Debio 0719) is a competitive, potent, and reversible antagonist to LPA1, LPA2, and LPA3, with Ki values of 0.34 μM, 6.5 μM, and 0.93 μM, respectively.