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Chemical Structure : HA-9104
Catalog No.: PC-21311Not For Human Use, Lab Use Only.
HA-9104 is a specific small molecule inhibitor of E2 conjugating enzyme UBE2F with IC50 of 33.29 uM for inhibition of cullin-5 neddylation, abrogates UBE2F-NEDD8 thioester formation and inhibits cullin-5 neddylation.
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HA-9104 is a specific small molecule inhibitor of E2 conjugating enzyme UBE2F with IC50 of 33.29 uM for inhibition of cullin-5 neddylation, abrogates UBE2F-NEDD8 thioester formation and inhibits cullin-5 neddylation.
HA-9104 inhibits cullin-5 neddylation via blocking the formation of UBE2F-NEDD8 thioester.
HA-9104 reduces UBE2F protein levels to selectively inhibits cullin-5 neddylation, causes accumulation of CRL5 substrate NOXA, in both dose- and time-dependent manners, with little to no effect on cullins 1-4, the other cullin family members.
HA-9104 reduces UBE2F protein via a mechanism of neither enhanced degradation, nor reduced translation.
HA-9104 significantly induces apoptosis via NOXA accumulation, induces G2/M arrest and triggers replication stress to delay DNA damage repair.
HA-9104 suppresses cancer cell growth and sensitizes cancer cells to radiation, inhibits in vivo tumor growth alone or in combination with radiation.
| M.Wt | 465.56 | |
| Formula | C28H27N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Tiantian Xu, et al. Signal Transduct Target Ther. 2022 Oct 17;7(1):354.
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