PNU-159682, a highly potent metabolite of the anthracycline nemorubicin (DNA topoisomerase II inhibitor) with outstanding cytotoxicity, is a potent ADCs cytotoxin. 了解更多
WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC50 of 122?±?30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells. 了解更多
NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3), and a cardiotonic agent with vasodilator properties. 了解更多
JTK-853 is a novel, non-nucleoside Hepatitis C Virus (HCV) polymerase inhibitor which shows effective antiviral activity in HCV replicon cells with EC50s of 0.38 and 0.035 ?M in genotype 1a H77 and 1b Con1 strains, respectively. 了解更多
Zaurategrast ethyl ester (CDP323), the ethyl ester prodrug of CT7758, is a α4β1/α4β7 integrin antagonist used for the treatment of inflammatory and autoimmune disorders. 了解更多
ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure. 了解更多
XEN723 is a novel and potent thiazolylimidazolidinone inhibitor of Stearoyl-CoA Desaturase (SCD1) with IC50s of 45 and 524 nM in mouse and HepG2 cell, respectively. 了解更多
Closthioamide is a potent inhibitor of bacterial DNA gyrase and highly active against Ec, MRSA, VRE and Mv), with MICs of 9.00 μM, 0.58 μM, 0.58 μM and 72.03 μM respectively. 了解更多
Tefinostat (CHR-2845) is a monocyte/macrophage-targeted pan HDAC inhibitor, cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Anti-monocytoid lineage leukaemias activity. 了解更多
AGI-25696 is a methionine adenosyltransferase 2A (MATA2 ) inhibitors useful for treatment of cancer. AGI-25696 blocks growth of MTAP-deleted tumors in vivo. 了解更多
Jennifer Kim, .et al. Intratarget Microdosing for Deep Phenotyping of Multiple Drug Effects in the Live Brain, Front Bioeng Biotechnol, 2022, Mar 18;10:855755 PMID: 35372313
AGI-24512 is a methionine adenosyltransferase 2A (MATA2 ) inhibitors useful for treatment of cancer. AGI-24512 blocks growth of MTAP-deleted cancer cells in vitro. 了解更多
Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively. 了解更多
Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC50 of 6.5 nM and Kd of 8 nM in Trypanosoma brucei. Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity. 了解更多
DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis. 了解更多
MGAT2-IN-1 is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively. 了解更多
Reproxalap (ADX-102) is a reactive aldehyde species (RASP) sequestering agent for the treatment of dry eye. Reproxalap (ADX-102) covalently binds aldehydes including malondialdehyde and 4-hydroxynonenal. 了解更多
N4-Acetylcytidine triphosphate is efficiently used as a substrate in T7 Polymerase-catalyzed in vitro transcription and can be incorporated into multiple templates. 了解更多
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