T6311

Bafetinib (INNO-406) (INNO-406) is an effective and specific dual Bcr-Abl/Lyn inhibitor (IC50: 5.8/19 nM), and no inhibition of the phosphorylation of the T315I mutant and less effective to c-Kit and PDGFR.

Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist that acts on D2 (Ki: 0.56 nM), D3 (Ki: 0.43 nM), and 5-HT2A (Ki: 0.6 nM) receptors, and also binds Alpha-1A adrenergic receptors. It can induce apoptosis, inhibit cancer cell proliferation, and is used to study psychiatric disorders, cancer, and inflammation.

CBP/p300-IN-15 (compound 13a) is a potent inhibitor of p300 (IC50: 2.5 nM) and CBP (IC50: 28.0 nM). It inhibits OVCAR-3 cells (EC50: 0.865 μM) and A2780 cells (EC50: 2.71 μM). CBP/p300-IN-15 can be used to study ovarian cancer.

Tubulin polymerization-IN-33, an [1,2] inhibitor of oxazoloisoindole microtubulin polymerization, is an effective anti-proliferative agent for NCI series cancer cells.

VEGFR-IN-3 (compound 3f), a VEGFR inhibitor, exhibits potent anticancer activity by inhibiting the growth of OVCAR-4 and MDA-MB-468 cancer cells with IC50 values of 0.29 and 0.35 μM, respectively. It has potential applications in cancer research [1].

HIV-1 inhibitor-21 (compound 9b) is a potent inhibitor of HIV-1 non-nucleoside reverse transcriptase (RT) with an IC50 of 0.55 μM. It inhibits both wild-type HIV-1 (EC50: 12.7 nM) and mutant virus strain K103N (EC50: 10.4 nM), demonstrating relatively low cytotoxicity (CC50 for MT-4: 10.2 μM).

ALK5-IN-7 is an effective inhibitor of ALK5. Transforming growth factor β (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation, and apoptosis through autocrine, paracrine, and endocrine pathways using complex receptor signaling pathways on the cell surface. ALK5-IN-7 has the potential to perform research on TGF-β-related diseases and conditions (including but not limited to tumor, fibrosis, inflammatory diseases, autoimmune diseases, etc.).

TXA6101 is an inhibitor of the bacterial protein FtsZ (filamentous temperature sensitive protein Z). TXA6101 inhibits bacterial division and has an MIC of 1 μg/mL against MRSA isolates expressing either the G193D or G196S mutant FtsZ and retains significant activity against the TXA707 resistant FtsZ mutant. TXA6101 can be used as a potential method of resistance to Gram-negative infections.

AMPK activator 7 (compound I-3-24) is an AMPK activator with an EC50 of 8.8 nM, useful in studies involving AMPK disorders such as type 2 diabetes, hyperglycaemia, metabolic syndrome, obesity, hypercholesterolaemia, and hypertension.

SOS1-IN-8 is an inhibitor of SOS1 and acts on SOS1-G12D (IC50: 11.6 nM) and SOS1-G12V (IC50: 40.7 nM).

NF-κB/MAPK-IN-1 is a potent dual inhibitor of the NF-κB and MAPK pathways with potential anti-inflammatory activity, inhibition of NO production, and inhibition of LPS-induced activation of iNOS, COX-2, ERΚ and P38. NF-κB/MAPK-IN-1 is used for the prevention and treatment of rheumatoid arthritis (RA).