MeOSuc-Gly-Leu-Phe-AMC is a peptide substrate of proteasomal[1].
Dovramilast (CC-11050) is an oral phosphodiesterase 4 (PDE4) inhibitor and can reduce the inflammatory response and improves Isoniazid (INH)-mediated bacillary clearance from the lungs. Dovramilast (CC-11050), as an adjunct, is used for the research of tuberculosis (TB)[1].
Trypsin Inhibitor, soybean is a potent and reversible inhibitor of trypsin[1].
Pedunculagin is a potent 5α-reductase type 1 inhibitor. Pedunculagin inhibits nitric oxide (NO), IL-6, IL-8 production. Pedunculagin decreases the protein expression of 5α-reductase. Pedunculagin shows anti-inflammatory activity[1].
CYP4Z1-IN-1 (compound 7c) is a potent CYP4Z1 inhibitor, with an IC50 of 41.8 nM. CYP4Z1-IN-1 decreases the expression of breast CSCs stemness markers, spheroid formation, and metastatic ability as well as tumor-initiation capability in a concentration-dependent manner in vitro and in vivo[1].
Calpain Inhibitor-1 (compound 36) is a potent and selective cysteine protease calpain 1 (Cal1) inhibitor (IC50=100 nM; Ki=2.89 μM)[1].
FCPR03 is a novel potent, selective PDE4 inhibitor with IC50 of 60, 31 and 47 nM for PDE4CAT (PDE4 catalytic domain), PDE4B1 and PDE4D7, respectively; displays >2,000-fold selectivity over other PDEs; effectively increases the production of cAMP, promotes CREB phosphorylation, and inhibits NF-κB activation both in vitro and in vivo; displays anti-neuroinflammation potential, promising antidepressant-like effects in vivo.
Acetyl-binankadsurin A (compound 5) is a lignan isolated from Kadsura longipedunculata. Acetyl-binankadsurin A has low inhibitory activity against HIV-1 protease, with IC50 >100 μg/mL[1].
Cilostamide is a selective and potent PDE3 inhibitor, with IC50s of 27 nM and 50 nM for PDE3A and PDE3B, respectively, and has antithrombotic and anti-intimal hyperplastic activity.
Plathymenin is a flavonoid that can be isolated from Nepalese propolis. Plathymenin is a potent inhibitor of 5-LOX[1][2].
Palmitic acid-d2-5 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
Sp-cAMPS, a cAMP analog, is potent activator of cAMP-dependent PKA I 和 PKA II. Sp-cAMPS is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS binds the PDE10 GAF domain with an EC50 of 40 μM[1][2][3].
FTI-277 is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.IC50 value:Target: FTase inhibitorin vitro: Treatment with FTI-277 (20 microM) for 48 h prior to irradiation led to a significant decrease in survival of radioresistant cells expressing the 24-kDa isoform (HeLa 3A) but had no effect on the survival of control cells (HeLa PINA). The radiosensitizing effect of FTI-277 is accompanied by a stimulation of postmitotic cell death in HeLa 3A cells and by a reduction in G(2)/M-phase arrest in both cell types [1]. Treatment of PC-3 cells with GGTI-298 and FTI-277 inhibited migration and invasion in a time- and dose-dependent manner [3].in vivo: FTI-277 treatment prevented increased PTP-1B and PTEN protein expression in burned mice as compared with vehicle alone. In contrast, FTI-277 did not significantly alter protein expression of PTP-1B and PTEN in sham-burned mice [2].