activating

TRAP-6 (Thrombin Receptor Activator Peptide 6)(2TFA) is an agonist of protease-activated receptor 1 (PAR1).

NAE-IN-M22 (NEDD8 inhibitor M22) is a selective, potent and reversible inhibitor of NEDD8 activating enzyme (NAE). NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.

Homoeriodictyol 7-O-β-D-glucoside (Homoeriodictyol 7-O-glucoside) is a natural product derived from Viscum coloratum (Kom.) Nakai and acts as an antagonist of platelet-activating factor (PAF).

Proteasome-activating peptide 1 TFA is a potent activator of the proteasome, enhancing chymotrypsin-like proteasomal catalytic activity and increasing proteolytic rates both in vitro and in culture. It also inhibits protein aggregation in cellular models of amyotrophic lateral sclerosis (ALS) [1].

Proteasome-activating peptide 1 enhances chymotrypsin-like proteasomal catalytic activity, boosting proteolytic rates both in vitro and within cultured cells. Additionally, it inhibits protein aggregation in a cellular model of amyotrophic lateral sclerosis [1].

PAR-2 Activating Peptide acetate (SLIGRL-NH2 acetate) is an agonist of Protease-Activated Receptor-2 (PAR-2).

Sperm-activating peptide 1 is a bioactive chemical.

Macrophage-activating lipopeptide 2 TFA (MALP-2 TFA) is a diacylglycerol lipopeptide and TLR-2/TLR-6 agonist that activates immune cell responses such as macrophages, upregulating TNF, IL-6, and PGE2 to induce local inflammation.

Macrophage-activating lipopeptide 2 (MALP-2) is a lipopeptide that acts as an agonist for Toll-like receptors TLR-2 and TLR-6. It enhances the phosphorylation of endothelial nitric oxide synthase (eNOS) and the release of nitric oxide (NO) by endothelial cells, thereby improving vasodilation. Additionally, MALP-2 increases the adhesion of leukocytes to the endothelium and enhances perfusion recovery and collateral growth in the hind limbs of hypercholesterolemic Apoe-deficient mice subjected to experimental femoral artery ligation (FAL).

48740 RP (RP 55779, (Rac)-RP-55778) belongs to synthetic compounds and is a platelet-activating factor (PAF) receptor antagonist with anti-inflammatory activity. This compound can be used in inflammation-related research, exerting its pharmacological effects through inhibition of the PAF/PAFR signaling pathway.

Pevonedistat (MLN4924) is a potent and selective NEDD8 activating enzyme (NAE) inhibitor (IC50=4.7 nM) with therapeutic potential for myelodysplastic syndromes (MDS) and antitumor activity.

Mezigdomide (CC-92480) is a potent, novel, selective and active cereblon E3 ubiquitin ligase modulator (CELMoD) that acts as a molecular glue. Mezigdomide has anti-myeloma activity. [1]

DF-1111301 is a novel anti-allergic compound with anti-histamine H1 and anti-PAF activity.

SDZ-62-434, a platelet-activating factor inhibitor with antitumor activity, inhibits bombesin- and platelet-derived growth factor-induced DNA synthesis in quiescent Swiss 3T3 cells, making it a potential candidate for studying leukemia, human xenograft colorectal cancer, and lung cancer.

Dersalazine (Dersalazine Free Base), an inhibitor of platelet-activating factor, exerts intestinal anti-inflammatory activity in different rodent types of colitis by down-regulating IL-17 expression, with potential efficacy in patients with ulcerative colitis.

Indole-3-carbinol (I3C), a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activation.

SCH-37370 is an effective and orally active dual antagonist of platelet-activating factor and histamine. Sch 37370 blocks the binding of [3H]pyrilamine to histamine-H1 receptors in rat brain membranes. Sch 37370 selectively inhibits PAF-induced aggregation of human platelets (IC50 : 0.6 mM) and also competes with PAF binding to specific sites in membrane preparations from human lungs (IC50 : 1.2 mM).

YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.

Nutlin-3b ((+)-Nutlin-3) is a p53/MDM2 antagonist or inhibitor (IC50: 13.6 μM), 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.

Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP) and soluble epoxide hydrolase (sEH) inhibitor, exhibiting marked anti-inflammatory efficacy and high target selectivity.

MD-224 is a highly potent and efficacious MDM2 degrader based on the proteolysistargeting chimera (PROTAC) concept,and as a new class of anticancer agent.

NSC232003 is a highly potent and cell-permeable inhibitor of [UHRF1].

TAS4464 hydrochloride is a highly potent and selective NEDD8 activating enzyme (NAE) inhibitor(IC50 of 0.955 nM).

Ubiquitination-IN-1 is an inhibitor of ubiquitination and Cksl-Skp2 protein-protein interaction (IC50: 0.17 μM).