T6241

Quetiapine hemifumarate (ICI-204636), an atypical antipsychotic, is used in the treatment of bipolar I mania, schizophrenia, bipolar II depression, bipolar I depression.

Hydroxyethylamine (Compd VII) is a SARS-CoV-2 3CLpro inhibitor with an IC50 of ~10 μM in a transmission assay, demonstrating significant antiviral effects.

CB1/2 agonist 4 (compound 24) is a CB1 full agonist (EC50: 15.09 nM) and a CB2 partial agonist (EC50: 1.16 nM). CB1/2 agonist 4 has significant anti-harm-sensing activity and also activates cannabinoid and TRPV1 receptors (IC50: 0.8 μM, EC50: 0.12 μM). , EC50: 0.12 μM).

FLT3-IN-12 is a selective, potent, orally active FLT3 kinase inhibitor that acts on FLT3-WT (IC50: 1.48 nM) and FLT3-D835Y (IC50: 2.87 nM). FLT3-IN-12 is more selective than c-KIT (>1000-fold). FLT3-IN-12 showed significant anti-AML effects, with an IC50 value of 0.75 nM for MV4-11 cells.

SARS-CoV-2 nsp13-IN-1 (compound C1) is a potent inhibitor of nsp13 (non-structural protein 13), selectively inhibiting nsp13 ssDNA+ATPase with an IC50 of 6 μM, but not ssDNA-ATPase, and can be used to study COVID-19.

Dyrk1A-IN-1 is a triple inhibitor of Dyrk1A kinase activity, tau aggregation, and α-syn oligomers, with an IC50 value of 119 nM for Dyrk1A kinase.

CBP/p300-IN-17 (compound 7) is a potent inhibitor of EP300/CBP HAT, with an IC50 of 0.18 μM for HAT EP300 and 0.69 μM for LK2 H3K27.

DX2-201 is a potent and selective inhibitor of oxidative phosphorylation (OXPHOS) complex I, with an IC50 of 312 nM, and it exhibits anticancer activity.

MELK-8a (NVS-MELK8a) is a potent and selective inhibitor of maternal embryonic leucine zipper kinase (MELK), with an IC50 of 2 nM and an IC50 of 0.42 μM in cellular assays. MELK is crucial in regulating mitosis in cancer cells.

hACC2-IN-1 is a potent inhibitor of acetyl coenzyme A carboxylase 2 (ACC2), exhibiting an IC50 of 2.5 μM for hACC2, and holds potential for obesity research.

Antifungal agent 13 demonstrates significant antifungal activity against Sclerotinia sclerotiorum, achieving an EC50 of 1.25 mg/L.