T6291

WZ4003, a highly selective NUAK kinase inhibitor, is with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2, respectively. It is no significant inhibition on 139 other kinases.

Antibacterial agent 62 is a novel redox cycle anti-tuberculosis compound exhibiting significant bactericidal activity against both growing and phenotypically resistant non-growing (nutrient deficient) bacteria.

Dalmelitinib is a selective, orally active c-Met kinase inhibitor (IC50: 2.9 nM) that binds the ATP-binding region of c-Met. Dalmelitinib induces phosphorylation of MET and partially or completely inhibits phosphorylation of AKT and ERK. dalmelitinib exhibits a potent inhibitory effect on the proliferation of cancer cells (c-Met oncogene amplification) and can be used in cancer research (e.g. non-small cell lung cancer).

PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50 values of 226 nM for PI3Kα, 279 nM for PI3Kβ, 467 nM for PI3Kγ, 29 nM for PI3Kδ, and 1.3 nM for HDAC1. PI3K/HDAC-IN-2 is selective for PI3Kδ and class I and IIb HDACs, exhibiting significant anticancer effects.

Piroxicam cinnamate (Cinnoxicam), a cyclooxygenase (COX) inhibitor with anti-inflammatory properties, is used to study inflammatory degenerative bone and joint diseases, rheumatic diseases, and varicocele-related oligospermia.

NSC 828467 is one of the top five CA-IX inhibitors with significant in vitro anticancer activity (IC50: 27.2 nM).

Dot1L-IN-7 (compound 25) is a selective and potent inhibitor of telomere silencing 1-like protein (DOT1L) with an IC50 of 1.0 μM. It selectively kills MLL-AF9 cells without affecting the growth of E2A-HLF cells.

GEM144 is a dual inhibitor of DNA polymerase α (POLA1) and HDAC 11. GEM144 induces p53 acetylation, activates p21, arrests the cell cycle in the G1/S phase, and induces apoptosis.

MIR002 is a potent, orally active dual inhibitor of DNA polymerase α (POLA1) and HDAC 11 with significant in vivo antitumor activity. p53 acetylation, p21 activation, cell cycle arrest in G1/S phase, and apoptosis induction.

GPR84 Antagonist 3 (compound 42), a potent inhibitor of the G-protein-coupled receptor 84 (GPR84), exhibits a pIC50 value of 8.28, indicating strong antagonistic activity by inhibiting GTPγS. Additionally, it possesses a favorable pharmacokinetic profile, suitable for further research and development [1].

CDK9-IN-13 is a potent and selective CDK inhibitor (IC50<3 nM). CDK9-IN-13 has a very short half-life in rodents.