Chemical Structure : UM130646
CAS No.:
UM130646
(UM 130646, UM0130646)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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640.54
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Formula
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C30H30Cl2F3N3O3S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Benoit Pelletier, et al. ACS Chem. Biol. 2023.
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