Drug Derivative Inhibitor

(1R,9R)-Exatecan mesylate ((1R,9R)-DX8951f) is a non-prodrug camptothecin derivative and a potent topoisomerase I inhibitor (IC₅₀=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1R,9R)-Exatecan mesylate is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia. The low-activity isomer of (1R,9R)-Exatecan mesylate is (1S,9R)-Exatecan mesylate (HY-13631I).

Petunidin chloride is an anthocyanin and also a pentoside (PEN) synthesis inhibitor. Petunidin chloride directly inhibits the synthesis of PEN without degrading or sequestering already synthesized PEN. Petunidin chloride can be used in studies related to PEN accumulation and advanced glycation associated with schizophrenia.

Larubrilstat is a vascular non-inflammatory molecule-1 (VNN1) inhibitor.

KP-10614 is a potent, orally active platelet aggregation inhibitor. KP-10614 inhibits platelet aggregation induced by ADP with IC₅₀ of 1 nM. KP-10614 causes dose-dependent inhibition of ex vivo platelet aggregation in rats. KP-10614 shows antithrombotic effects in various thrombosis models. KP-10614 can be used for thrombotic diseases research.

Kaempferol 3-rungioside is a glycoside derivative of Kaempferol (HY-14590).

Anticancer agent 208 (C014) is an anticancer agent that can be used to inhibit cancer or prevent its recurrence.

Anticancer agent 224 (Compound 16) is an anticancer agent that can effectively inhibit the growth of central nervous system (CNS), kidney and breast cancer cell, with a GI₅₀ value ranging from 0.6 to 12.8 μM.

Argimesna ethanesulfonate is a uroprotective agent. Argimesna ethanesulfonate is promising for research of hemorrhagic cystitis in cancer chemotherapy.

2-Mercaptopyridin-3-ol (3-HPT) is a natural product with strong metal coordination ability. 2-Mercaptopyridin-3-ol can be used as a metal enzyme inhibitor.

Anidoxime hydrochloride is an Amidoxime derivative, and an orally active analgesic agent. Anidoxime hydrochloride can be used for the research of post-surgical pain.

(1R,9R)-Exatecan ((1R,9R)-DX8951f) is a non-prodrug Camptothecin (HY-16560) derivative and a potent topoisomerase I (Topo I) inhibitor (IC₅₀=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1R,9R)-Exatecan is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia. The low-activity isomer of (1R,9R)-Exatecan is (1S,9R)-Exatecan (HY-13631I).

β-Ionone acid, an analog of β-Ionone, is a promising anticancer agent.