t-448

T-448 is a specific, orally active, and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) with an IC50 of 22 nM.

T-448 free base, an orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), has an IC50 of 22 nM.

(iso)-T 448 is a rotary isomer of T 448. T-448 is a potent lysine-specific demethylase 1 (LSD1) inhibitor that induces the methylation of H3K4 in rat neurons.

Tucidinostat (Chidamide) is an effective and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8/11 (IC50: 733/432 nM), and shows no effect on HDAC4/5/6/7/9.

TNP (IP3K Inhibitor) is a cell-permeable inhibitor of IP6K1 and IP3K, with IC 50 values of 0.55 μM and 10.2 μM for IP6K1 and IP3K, respectively. TNP binds to the ATP-binding sites of both enzymes [1].

GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).

Vardenafil dihydrochloride (Levitra) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

CC-671 is a dual inhibitor of TTK protein kinase (IC50: 0.005 μM) and CLK2 (IC50: 0.006 μM).

1,7-Dihydroxy-2,3-methylenedioxyxanthone exhibits antiulcerogenic, anti-oxidation, and antihyperalgesic activities and can inhibit carrageenan-induced hyperalgesia.

Lazertinib (GNS-1480) is an effective, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively.

iCRT 14 is a novel and potent inhibitor of β-catenin-responsive transcription (CRT) with an IC50 of 40.3 nM in assays of Wnt pathway activity.

AKT-IN-1 (AZD-26) is an allosteric AKT inhibitor (IC50: 1.04 μM).

TAK-448 is an investigational oligopeptide analog of kisspeptin and a potent agonist of the GPR54 receptor. In animals, acute TAK-448 administration stimulates LH/FSH release, whereas continuous sc exposure rapidly down-regulates the pituitary-gonadal axis, with rapid reduction of T levels in a dose-dependent manner. TAK-448 has exhibited potent antitumor activity in rat androgen-dependent prostate cancer models. Therefore, TAK-448 may be useful in the treatment of PC in humans..

Belrestotug (EOS-448), an antagonistic anti-TIGIT (VSIG9, VSTM3) fully human antibody, exhibits antineoplastic activity. Belrestotug is relevant for immuno-oncology investigations involving TIGIT-mediated immune checkpoint regulation, tumor immune microenvironment interactions, and T-cell functional modulation.