Drug intelligence / Profile preview

debromohymenialdisine

Development stage
Preclinical
Modality
Small Molecules
01

Overview

Debromohymenialdisine is a marine-derived pyrrole alkaloid, classified as a small molecule, originally isolated from sponges such as Stylissa massa and Axinella carteri. It acts primarily as an inhibitor of checkpoint kinases Chk1 and Chk2, with IC50 values of approximately 3–3.5 μM, thereby blocking the G2 DNA damage checkpoint in cells. Additionally, it inhibits MAP kinase kinase 1 (MEK1) with moderate potency (IC50 ≈ 881 nM), protein kinase C (PKC), and has been reported to have anti-inflammatory effects by downregulating NF-kB signaling and promoting Nrf2/HO-1 pathways. Debromohymenialdisine does not inhibit ATM or ATR kinases. Its biological activities include cytotoxicity against cancer cells, anti-inflammatory effects relevant to diseases like inflammatory bowel disease, potential anti-Alzheimer’s activity, insecticidal properties, and possible use as an antineoplastic agent[3][4][5][7][8].

Other names
(Z)-Debromohymenialdisine(Z)-2-DebromohymenialdisineDebromo Hymenialdisinedebromohymenialdesine
02

Targets

CHEK1 (Checkpoint kinase 1)NF-κBMEK1 (Dual specificity mitogen-activated protein kinase kinase 1)CHEK2 (Checkpoint kinase 2)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)PKC (Protein kinase C family)

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