necrosis

Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM). Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent.

PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 of 2.0 nM and Ki of 3.6 nM.

(S)-(+)-Rolipram ((+)-Rolipram) inhibits human monocyte cyclic AMP-specific PDE4 with an IC50 of 0.75 μM and exhibits anti-inflammatory and anti-depressant activity in the central nervous system, though it is less potent than its R enantiomer.

Necrosulfonamide ((E)-Necrosulfonamide) is a necroptosis inhibitor that targets MLKL and is selective. Necrosulfonamide prevents the MLKL-RIP1-RIP3 necrosomal complex from interacting with its downstream effectors.

Fasentin (N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide) is an inhibitor of GluT1.

PF-543 hydrochloride (PF-543) inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.

R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist that exhibits heightened selectivity for TNFα.

Resatorvid (TAK-242), a selective Toll-like receptor 4 (TLR4) inhibitor, binds directly to Cys747 to prevent TLR4-TIRAP interaction, thereby blocking downstream signaling. Resatorvid exhibits antitumor, anti-inflammatory, and neuroprotective activities.

SR-318 is a potent and highly selective inhibitor of p38 MAPK, demonstrating IC50 values of 5 nM for p38α, 32 nM for p38β, and 6.11 μM for p38α/β. It possesses both anti-cancer and anti-inflammatory activity.

Naphazoline hydrochloride (Naphazoline HCl) is an adrenergic vasoconstrictor agent used as a decongestant.

Theophylline monohydrate (Quibron) appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Theophylline monohydrate is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Physiologically, this agent relaxes the bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates the cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm.

Fisetin belongs to a group of natural flavonols with a variety of biological activities, including anti-inflammatory, antioxidant, anti-tumor, anti-aging and neuroprotective effects.

Muscone (3-Methylcyclopentadecanone) is an organic compound that is the primary contributor to the odor of musk.

Apremilast (CC-10004) (CC-10004) is a potent and orally active PDE4 (IC50=74 nM) with anti-inflammation activities.

VGX-1027 (GIT 27) is an isoxazole compound with various immunomodulatory properties.

BU 224 hydrochloride is a selective imidazoline I(2) binding site ligand and has antinociceptive and antidepressant-like activities.

Methylthiouracil is a thiourea-class antithyroid agent that inhibits the synthesis of thyroid hormones and is commonly used to treat hyperthyroidism. Studies have shown that Methylthiouracil can also suppress the production of TNF-α and IL-6, as well as inhibit the activation of NF-κB and ERK1/2. It can be used to induce hyperlipidemia and neurological disorder models.

(+)-Shikonin (Anchusa acid) is a natural product, a TMEM16A chloride channel inhibitor (IC50=6.5 μM) and selective PKM2 inhibitor. (+)-Shikonin exhibits antitumor, anti-inflammatory and wound healing activities.

UCB-9260 inhibits TNF signaling by stabilizing an asymmetric form of the trimer.

C 87 is a small-molecule TNF-α inhibitor. C 87 directly binds to TNFα, potently inhibits TNF-α-induced cytotoxicity (IC50 = 8.73 μM), and effectively blocks TNF-α-triggered signaling activities.

CJ-42794 (CJ-042794) is a selective antagonist of the prostaglandin E receptor subtype 4 (EP4), inhibiting [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5. It exhibits a binding affinity that is at least 200-fold more selective for the human EP4 receptor than for other human EP receptor subtypes (EP1, EP2, and EP3) (IC50: 8.5 (pKi)).

Eucalyptol, a natural monoterpenoid and cyclic ether found in eucalyptus species, effectively controls excessive airway mucus secretion and asthma by inhibiting pro-inflammatory cytokines. It serves as an efficacious treatment for non-purulent sinusitis, reducing inflammation and pain when applied topically, and demonstrating leukemic cell-killing capabilities in vitro.

Bioymifi (DR5 Activator) is an effective activator of the TRAIL receptor DR5, binding to the extracellular domain (ECD) of DR5 with a Kd of 1.2 μM. Bioymifi can serve as a novel mimetic of TNF-related apoptosis-induced ligand (TRAIL), inducing DR5 aggregation as a sole inducer, and stimulating cell apoptosis.

LY303511, an inactive analogue of LY294002, is a mTOR inhibitor and no inhibition for PI3-K.