T6214

Emtricitabine is a nucleoside reverse transcriptase inhibitor with anti-human immunodeficiency virus (HIV) and hepatitis B virus activity, with an EC50 value of 0.01 µM in PBMC cells, and can be used to study HIV infection.

HF50731 is a potent antagonist of CXCR4. HF50731 has a strong binding affinity for CXCR4 (IC50: 19.8 nM). HF50731 utilizes the CXCR4 co-receptor and effectively inhibits calcium mobilization (IC50: 119.2 nM), cell migration (IC50: 621.4 nM) and HIV-1 infection (IC50: 1.5 nM). IC50: 1.5 nM).

RBP4 ligand-1 is a non-retinoid ligand for retinol-binding protein 4 (RBP4). It exhibits hRBP4SPA IC50 and RBP4-TTR FRET IC50 values of 0.23±0.11 μM and 0.13±0.12 μM, respectively, in radioligand binding and FRET assays. The measured concentration was 0.12 μM.

COX-2-IN-17 is a potent, blood-brain barrier permeable COX-2 (cyclooxygenase-2) inhibitor (IC50: 0.02 μM) with anti-inflammatory and analgesic activity.

LP-922761 hydrate is a selective, potent, orally active AAK1 inhibitor with IC50 values of 4.8 nM and 7.6 nM in enzyme and cellular assays, respectively. LP-922761 hydrate inhibits BMP-2 inducible protein kinase (BIKE) (IC50: 24 nM). 922761 hydrate has no significant effect on cellular GAK, opioids, adrenergic α2 or GABAa receptors.

PXYD3 is a ribosomal protein S1 (RpsA) antagonist that targets RpsA-CTD [Kd: 5.66 μM] and RpsA-CTD Δ438A [Kd: 6.91 μM], with RpsA being crucial for the translocation of Mycobacterium tuberculosis (Mtb).

PXYD4 is a ribosomal protein S1 (RpsA) antagonist that binds to RpsA-CTD (Kd: 3.24 μM) and RpsA-CTD Δ438A (Kd: 1.64 μM). RpsA is critical for the translocation of Mycobacterium tuberculosis (Mtb).

DprE1-IN-4 is a potent, non-covalent inhibitor of DprE1 (IC50: 0.90 μg/mL). DprE1-IN-4 has acceptable pharmacokinetic properties and has a significant bactericidal effect in a mouse model of acute tuberculosis.

NW 1028 is a potent inhibitor of VCP/p97. NW 1028 selectively acts on the ND1L domain of p97 and inhibits the degradation of p97-dependent reporter genes. NW 1028 has a regulatory effect on the mitotic spindle.

ALM301 is a highly specific, orally active AKT inhibitor that acts on AKT1 (IC50: 0.13 μM), AKT2 (IC50: 0.09 μM) and AKT3 (IC50: 2.75 μM). ALM301 inhibits AKT phosphorylation in vitro and has a regulatory effect on downstream signalling. ALM301 exhibits inhibitory effects on cancer cell proliferation and tumor growth.