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Chemical Structure : HY041004
Catalog No.: PC-21610Not For Human Use, Lab Use Only.
HY041004 is the first small molecule inhibitor of deubiquitinase Josephin Domain-containing protein 2 (JOSD2) with IC50 of 0.26 uM for JOSD2 catalytic activity inhibition.
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HY041004 is the first small molecule inhibitor of deubiquitinase Josephin Domain-containing protein 2 (JOSD2) with IC50 of 0.26 uM for JOSD2 catalytic activity inhibition.
HY041004 (2 uM) shows potent inhibitory effect against JOSD2 catalytic activity as 86.14% in in vitro ubiquitin-AMC assays, also robustly blocks the loss of K6-linked polyubiquitination on LKB1 caused by JOSD2 in cellular assays.
HY041004 also exhibits on-target engagement in cancer cells in cellular thermal shift assay.
HY041004 displays a less but comparable inhibition on JOSD1 (IC50=0.47 μM) and much weaker activity against other two MJDs Ataxin-3 and Ataxin-3L with IC50 of 5.4 and 12.8 μM, respectively.
HY041004 displays potent anticancer effects in NSCLC cell in vitro, which is dependent on JOSD2-LKB1 axis.
HY041004 (orally, twice daily, 50 mg/kg and 100 mg/kg) significantly suppresses tumor growth and induced intratumor cell apoptosis on NCI-H1299 xenografted tumors.
| M.Wt | 342.71 | |
| Formula | C16H8ClFN4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Liu, J. et al. The invention discloses a naphthoquinone triazole core skeleton derivative compound, a preparation method and application thereof. China patent CN110218198A (2019).
2. Tao Yuan, et al. Signal Transduct Target Ther. 2024 Jan 5;9(1):11.
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