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Target Protein Ligand-Linker Conjugates 4 is a compound formed by connecting a target protein ligand with a linker. It is used in the synthesis of PROTACs, such as PROTAC SMARCA2 degrader-21.

Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and a potent chemosensitizer that enhances the number of DNA double-strand breaks induced by Doxorubicin. It serves as an effective multidrug resistance (MDR) inhibitor, demonstrating inhibitory activity against P-glycoprotein (P-gp) mediated drug efflux. Multi-target kinase inhibitor 4 can be encapsulated in PEG-coated lipid nanoparticles.

Multi-target Pt (IV) is an antitumor agent that inhibits the phosphorylation of IKKβ, IκBα, and NF-κB p65, as well as the nuclear translocation of NF-κB p65, ultimately blocking the NF-κB signaling pathway.

Multi-target kinase-IN-5 (Compound 23) is an orally active ERK1/2 inhibitor with IC50 values of 3.04 nM and 1.57 nM, respectively. It notably suppresses cancer cell proliferation, migration, and invasion, while inducing apoptosis and cell cycle arrest. By inhibiting the phosphorylation of ERK1/2 and downregulating the activity of its downstream substrate RSK, Multi-target kinase-IN-5 exhibits antitumor effects. This compound can be utilized in cancer research.

Multi-target kinase-IN-6 is a multi-target kinase inhibitor. It can inhibit cardiac RyR2 and NaV1.5 channels while stimulating the activity of the SERCA2a pump. Multi-target kinase-IN-6 is applicable in research on cardiovascular diseases, including heart failure.

Compound 5K (Multi-target kinase inhibitor 2) is a multi-targeted kinase inhibitor demonstrating activity against EGFR, Her2, VEGFR2, and CDK2 with IC50 values between 40 to 204 nM. It exhibits cytotoxic effects on HepG2, HeLa, MDA-MB-231, and MCF-7 cell lines, with IC50 values of 41, 57, 51, and 59 μM, respectively. Additionally, it induces cell cycle arrest and apoptosis specifically in HepG2 cells.

3BDO is an activator of mTOR. It can also inhibit autophagy..

Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.

Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.

AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.

MHY1485 is an mTOR activator that is cell-permeable. MHY1485 inhibits autophagosome and lysosome fusion, leading to accumulation of LC3II proteins and increased autophagosomes, thereby inhibiting cellular autophagy.

Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.

Salidroside is a bioactive phenolic glycoside compound isolated from Rhodiola rosea and is a prolyl endopeptidase inhibitor. Salidroside can alleviate cachexia symptoms in a tumor cachexia mouse model by activating mTOR signaling and protect dopaminergic neurons by enhancing PINK1/Parkin-mediated mitochondrial autophagy. Salidroside can also inhibit the growth of cancer cells by regulating the CDK4-cyclin D1 pathway to block the G1 phase and/or regulating the Cdc2-cyclin B1 pathway to block the G2 phase.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis/erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.

CPI-0610 carboxylic acid is an effective and selective small molecule inhibitor of bromine domain and outer end (BET) protein as a ligand of PROTAC target protein. CPI-0610 carboxylic acid may have anticancer and anticancer activities.

mTOR inhibitor-3 is a selective mTOR inhibitor (Ki= 1.5 nM). mTOR inhibitor-3 inhibits mTORC1 and mTORC2 in cellular and in vivo experiments.

NV-5138 is a selective, orally active intracerebral mTORC1 agonist that binds to Sestrin2. It is a leucine analog. It can be used in biological studies of antidepressants.

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

BGT226 (NVP-BGT226) is a novel dual PI3K/mTOR inhibitor, targeting PI3K α, β, and γ with IC50 values of 4 nM, 63 nM, and 38 nM, respectively.

WYE-125132 (WYE-132 (WYE-125132)) is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.

GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.

WAY-600 is a potent, ATP-competitive, and selective inhibitor of mTOR with an IC50 of 9 nM; it blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308), and is selective for mTOR over PI3Kα (>100-fold) and PI3Kγ (>500-fold).

PF-04979064 is a potent and selective PI3K and mTOR dual kinase inhibitor, with Ki values of 0.13 nM and 1.42 nM, respectively.