Chemical Structure : UBA5 inhibitor Compound 8.5
CAS No.:
1831169-11-9
UBA5 inhibitor Compound 8.5
(UBA5-IN-1)
货号: PC-24868Not For Human Use, Lab Use Only.
UBA5 inhibitor Compound 8.5 (UBA5-IN-1) is a potent, selective UFM1 activating E1 enzyme UBA5 inhibitor with IC50 of 4.0 uM (inhibition of UFM1 transthiolation from UBA5 to UFC1).
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
UBA5 inhibitor Compound 8.5 (UBA5-IN-1) is a potent, selective UFM1 activating E1 enzyme UBA5 inhibitor with IC50 of 4.0 uM (inhibition of UFM1 transthiolation from UBA5 to UFC1).
Compound 8.5 displays 20-fold selectivity for UBA5 over both UAE (IC50 = 78.5 μM) and NAE (IC50 = 66.8 μM), also shows no significant inhibition of ATP binding to 97 human kinases.
Compound 8.5 might bind an allosteric site on the UBA5 homodimer.
Compound 8.5 inhibits UBA5 non-competitively with respect to ATP.
Compound 8.5 suppressed the proliferation of Sk-Luci6 cancer cells that express high levels of UBA5 (at concentrations above 50 μM) while no effect was observed on A549 cancer cells or MRC9 lung fibroblasts (up to 200 μM).
Compound 8.5 demonstrated selective anti-proliferative effects on cells expressing higher levels of UBA5.
物理化学性质&存储条件
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分子量
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912.16
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分子式
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C26H40F6N10O11S2Zn
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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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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C(S(=O)(=O)[O-])(F)(F)F.C(CCCCCNC(=O)[C@H]1O[C@H]([C@H](O)[C@@H]1O)N2C=3C(N=C2)=C(N)N=CN3)(=O)[N]45[Zn+2]67[N](CC4)(CC[N]6(CC[N]7(CC5)[H])[H])[H]
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参考文献
1. da Silva SR, et al. Bioorg Med Chem Lett. 2016 Sep 15;26(18):4542-4547.
2. Zou Y, et al. Proc Natl Acad Sci U S A. 2025 Jul 8;122(27):e2500562122.
