Drug intelligence / Profile preview

HAC-Y6

Development stage
Preclinical
Lead developer
China Medical University
Modality
Small Molecules
Administration
In Vitro (cell Studies)
01

Overview

**HAC-Y6** is a novel synthetic small-molecule compound described as 6-acetyl-9-(3,4,5-trimethoxybenzyl)-9H-pyrido[2,3-b]indole. It acts as a potent microtubule-depolymerizing agent, causing microtubule fragmentation and inhibition of α- and β-tubulin assembly, similar to colchicine. HAC-Y6 induces cell cycle arrest at the G2/M phase and triggers apoptosis through both intrinsic (mitochondrial) and extrinsic (death receptor 4) pathways. Molecular mechanisms implicated include activation of Bax and caspases 3/8/9, inactivation of Bcl-2 and Bcl-xL, upregulation of BubR1, and inhibition of HSP90, with additional inactivation of aurora A and aurora B kinases. Preclinical studies show antitumor activity against human hepatocellular carcinoma and colon carcinoma cell lines[1][4].

Other names
6-acetyl-9-(3,4,5-trimethoxybenzyl)-9H-pyrido[2,3-b]indole
02

Targets

TNFRSF10A (Death receptor 4)BCL2L1 (B-cell lymphoma-extra large protein)AURKB (Aurora kinase B)BAX (Apoptosis regulator BAX)AURKA (Aurora kinase A)TUBB (Tubulin (alpha and beta subunits))BUB1B (Mitotic checkpoint serine/threonine-protein kinase BUB1 beta)

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