T6196

PP1 (AGL 1872), a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.

Fluconazole (mesylate) is a triazole antifungal drug used for the treatment and prevention of both superficial and systemic fungal infections.

Pyruvate Carboxylase-IN-2 is a natural analog of erianin. Pyruvate Carboxylase-IN-2 (compound 29) is a potent inhibitor of pyruvate carboxylase (PC). In cell lysate-based and cell-based PC activity assays, Pyruvate Carboxylase-IN-2 shows IC 50 s of 0.065 and 0.097 μM, respectively. Pyruvate Carboxylase-IN-2 mediates the anticancer effect in human hepatocellular carcinoma (HCC).

PARP-1/HDAC-IN-1 is an effective dual inhibitor of PARP-1 and HDAC6, with IC50 values of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 exhibits anti-cancer, anti-migration, and anti-angiogenesis activities.

SOS1-IN-3 is an effective inhibitor of SOS1 (son of sevenless homolog 1) (IC50=5 nM). SOS1-IN-3 shows antitumor activity.

RXFP3/4 agonist 2 is a potent, non-peptidic bis-RXFP3/4 agonist that facilitates the interaction between RXFP3 and β-arrestin-2 and is useful for studying diseases caused by metabolic abnormalities.

SphK1-IN-1 is an inhibitor of SphK1 with anti-tumor activity. SphK1-IN-1 inhibits the ATPase of SphK1, IC50=2.48 μM. SphK1-IN-1 has the value of cancer research.

PI3K-IN-26 is an effective PI3K inhibitor. PI3K-IN-26 inhibits the proliferation of SU-DHL-6 cells, IC50= 36 nM.

PI3Kα-IN-7 (Compound A12) is a potent inhibitor of PI3Kα and PI3Kβ, capable of reducing mitochondrial membrane potential in cancer cells and inducing apoptosis.

PD-1/PD-L1-IN 6 (compound A13) is a potent inhibitor of PD-1/PD-L1 interaction (IC50 = 132.8 nM) with outstanding immunoregulatory activity. In a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, PD-1/PD-L1-IN 6 significantly elevates interferon-γ secretion without significant toxic effects. Additionally, in a T cell-tumor co-culture model, PD-1/PD-L1-IN 6 restores the immune response.

AChE/BChE-IN-10 is a potent dual inhibitor of AChE and BChE with IC50 values of 0.176, and 0.47 μM, respectively. AChE/BChE-IN-10 exhibits good blood brain barrier permeability. AChE/BChE-IN-10 can inhibit Aβ-aggregation.