T6270

Trichostatin A (TSA), a natural derivative of diene isohydroxamic acids, is a specific and reversible histone deacetylase inhibitor (IC50=1.8 nM) that induces hyperacetylation of core histones to regulate chromatin structure.

Senexin C is a novel orally active and specific CDK8/19 inhibitor with potential anticancer activity.Senexin C is more metabolically stable and potent than Senexin B. Senexin C inhibits the growth of MV4-11 leukaemia cells.

CBP/p300-IN-16 (compound 1) is a potent inhibitor of EP300/CBP HAT, targeting HAT EP300 with an IC50 of 0.61 μM and LK2 H3K27 with an IC50 of 2.24 μM.

Dihydropteroate synthase-IN-1 (compound 5g) is a potent inhibitor of dihydropteroate synthase (DHPS) and cytochrome P450, and can be used as a diagnostic radiographic material.

NTPDase-IN-2 (compound 5g) selectively inhibits NTPDase-2 and NTPDase-8 with IC50 values of 0.04 µM and 2.27 µM, respectively, and exhibits non-competitive inhibition toward h-NTPDase-1 and h-NTPDase-2, with a Km of 74 µM for h-NTPDase-2. This compound is applicable in researching cancer, immunological disorders, and bacterial infections [1].

HBV-IN-23 (Compound 5k) is an inhibitor of HBV DNA replication with an IC50 of 0.58 μM, inhibiting both drug-sensitive and drug-resistant strains. It induces apoptosis in HepG2 cells and demonstrates anti-hepatocellular carcinoma (HCC) effects.

NSD2-IN-1 (compound 38) is a potent and highly selective inhibitor of NSD2-PWWP1 (nuclear receptor-binding SET domain 2-PWWP1), with an IC50 value of 0.11 μM. By binding to NSD2-PWWP1, NSD2-IN-1 influences gene expression regulated by NSD2, resulting in apoptosis and cell cycle arrest [1].

RTI-7470-44 is a potent and selective human trace amine-associated receptor 1 (hTAAR1) antagonist (IC50: 8.4 nM) that crosses the blood-brain barrier. RTI-7470-44 increases the spontaneous firing rate of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain in mice. RTI-7470-44 can be used to study schizophrenia, drug addiction and Parkinson's disease (PD).

Antimicrobial agent-4 (compound 6a) is a potent antimicrobial agent with a high binding capacity of 10.0 kcal/mol for the target enzyme, demonstrating significant activity against microbial pathogens.

HDAC-IN-37 is a potent inhibitor of HDAC, targeting HDAC1 (IC50: 0.0551 μM), HDAC3 (IC50: 1.24 μM), HDAC8 (IC50: 0.948 μM), and HDAC6 (IC50: 34.2 μM). It slowly induces histone acetylation, prevents the transition from G1 to S phase, and induces early apoptosis.

EBOV-GP-IN-1 (Compound 28) is a potent inhibitor of Ebola virus entry, targeting the Ebola virus envelope glycoprotein (EBOV-GP) with an IC50 of 0.05 μM.