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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Ubiquitin-conjugating Enzyme (E2)-UM130646
UM130646

Chemical Structure : UM130646

CAS No.:

UM130646 (UM 130646, UM0130646)

货号: PC-20652Not For Human Use, Lab Use Only.

UM130646 (UM 130646) is a specific small molecule E2 enzyme UBCH10 inhibitor with IC50 of 20.3 uM in TR-FRET UBCH10 autoubiquitination assays, inhibits UBCH10 E2 activity and antagonizes APC/C-mediated substrate degradation.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

UM130646 (UM 130646) is a specific small molecule E2 enzyme UBCH10 inhibitor with IC50 of 20.3 uM in TR-FRET UBCH10 autoubiquitination assays, inhibits UBCH10 E2 activity and antagonizes APC/C-mediated substrate degradation.
UM130646 does not affect the ubiquitin-conjugating activity of UBE2S and UBE2T in TR-FRET assays at 50 uM, also shows no detectable effect on the formation of UBE1-ubiquitin or UBCH10-ubiquitin thioester formation.
UM130646 treatment (50 uM) led to a clear accumulation of endogenous securin levels in HeLa cells.
UBCH10 is a specific E2 for the APC/C E3 ligase, a key regulator of cell cycle progression.

物理化学性质&存储条件

分子量 640.54
分子式 C30H30Cl2F3N3O3S
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

O=C1CC(C2=CC=CS2)CC3=C1C(C4=CC=C(C(F)(F)F)C=C4)N(CCOCCOCCN)C5=CC(Cl)=C(Cl)C=C5N3

参考文献

1. Benoit Pelletier, et al. ACS Chem. Biol. 2023.

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