ROS Kinase Activator

Melamine is an orally active inducer of Apoptosis. Melamine induces animal disease models. Melamine affects the activity of Sertoli cell and can be used for research on male reproductive function. Melamine also has neurotoxicity and nephrotoxicity. Melamine induces cognitive impairment and acute kidney injury models. Melamine can also be used to induce bladder cancer and urinary stone models.

PROTAC GPX4 degrader-4 is a GPX4 PROTAC degrader (DC₅₀: 5.32 nM). PROTAC GPX4 degrader-4 inhibits the activity of RT4, T24, and J82 cancer cells (IC₅₀ values are 0.09, 2.97, and 7.58 μM, respectively). PROTAC GPX4 degrader-4 increases lipid ROS levels and induces ferroptosis in T24 and RT4 cells. PROTAC GPX4 degrader-4 has antitumor activity in T24 tumor-bearing BALB/c nude mouse model. PROTAC GPX4 degrader-4 can be used for bladder cancer research. (Pink: target protein ligand (HY-N0193); blue: E3 ligase ligand (HY-1035960); black: linker (HY-W013907); E3 ligase ligand + linker (HY-174087)).

Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a K_d value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model.

HS-291 is a HtpG inhibitor of Borrelia burgdorferi (Bb). HS-291 contains BX-2819 (high affinity for Bb HtpG), PEG linker, and Verteporfin (HY-B0146) (a photoactive toxin).HS-291 produces reactive oxygen species under light activation to oxidize HtpG and a discrete protein subset near chaperone proteins and can quickly and irreversibly inactivate Bb.

Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC₅₀s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca²⁺ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model.

Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC₅₀ of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca²⁺ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model.

Topo I/II-IN-2 (Compound 3g) is an inhibitor of Topo I and Topo II. Topo I/II-IN-2 inhibits NCI-H446 cells and NCI-H1048 cells with IC₅₀s of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial Apoptosis, mitochondrial dysfunction and activity generation. Topo I/II-IN-2 inhibits the PI3K/Akt/mTOR pathway. Topo I/II-IN-2 prevents SCLC (small cell lung cancer) cell proliferation, invasion, and migration in vitro. .

BRD5459 is a ROS chemical probe. BRD5459 can increase ROS, a marker of oxidative stress in cells, without causing cell death.