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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Ubiquitin-conjugating Enzyme (E2)-HA-9104
HA-9104

Chemical Structure : HA-9104

CAS No.: 2412367-83-8

HA-9104 (HA9104, iV26-9-10-4)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 465.56
分子式 C28H27N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(E)-N-(4-(4-(4-methylbenzoyl)piperazin-1-yl)phenyl)-3-(1H-pyrrolo[2,3-b]pyridin-3-yl)acrylamide

参考文献

1. Tiantian Xu, et al. Signal Transduct Target Ther. 2022 Oct 17;7(1):354.

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