您的位置:首页 > 产品中心 > 1319207-44-7, Cdc34 Inhibitor, CC0651-CAS 1319207-44-7-Calbiochem
Cdc34 Inhibitor, CC0651-CAS 1319207-44-7-Calbiochem
产品编号: | 4083508 |
规格: | A cell-permeable, selective allosteric inhibitor of E2 ubiquitin-conjugating enzyme Cdc34 (IC50 = 2.5 μM in a Sic1-SCFCdc4 assay). |
CAS NO: | 1319207-44-7 |
包装规格: | 10 MG |
产品类别: | 进口试剂 |
品牌: | Sigma-Aldrich |
优惠价: | 立即咨询 |
产品价格查看更多规格...
产品编号 | 包装单位 | 单价(元) | 国内现货 | 国外库存 | 询价单 |
4083508 | 10 MG | 3250 |
产品别名
1319207-44-7
Cdc34 Inhibitor, CC0651-CAS 1319207-44-7-Calbiochem
4,5-Dideoxy-5-(3',5'-dichloro-4-biphenylyl)-4-((methoxyacetyl)amino)-L-arabinonic acid, (2 R,3 S,4 S)-5-(3',5'-Dichloro-(1,1'-biphenyl)-4-yl)-2,3-dihydroxy-4-(2 methoxyacetamido)pentanoic acid, Cdc34A Inhibit
基本信息
Empirical Formula【经验(实验)分子式】 | C20H21Cl2NO6 |
Molecular weight | 442.29 |
General description【一般描述】 | A cell-permeable biphenylylpentanoic acid compound that acts as a selective allosteric inhibitor of E2 ubiquitin-conjugating enzyme Cdc34 (IC50 = 2.5 µM in a Sic1-SCFCdc4 assay) without affecting the activities of E1 or E3 ligases. Reported to act by trapping a weak interaction between ubiquitin and the E2 donor ubiquitin-binding site and may serve as a molecular bridge between Cdc34A and ubiquitin. Binds to Cdc34ACAT alone with an EC50 value of 267 µM, but in the presence of ubiquitin, this affinity is significantly increased (EC50 = 19 µM). Does not disrupt the interaction of Cdc34A with the RING domain of Rbx1 and is suggested to even moderately stabilize this interaction. Shown to inhibit p27Kip1 ubiquitination (IC50 = 1.72 µM) and reduce PC-3 cancer cells proliferation (~30 µM). Please note that the molecular weight for this compound is batch-specific due to variable water content. A cell-permeable and aqueous soluble (~ 1 mg/mL or 2.26 mM at pH 7.4) biphenylylpentanoic acid that selectively inhibits human, but not yeast, E2 Ub-conjugating enzyme Cdc34- dependent substrates ubiquitinations in p27kip1-SCFSkp2, Sic1-SCFCdc4 (IC50 = 1.72 & 2.5 µM, respectively), Cyclin E-SCFFbw7, IκBα-SCFβTrCP ubiquitination assays and induces cellular p27kip1 and cyclin E accumulation (30 µM for 16 h in PC-3 cultures), displaying no affinity or inhibitory activity against other E1 (Uba1), E2 (Cdc34B/Ube2R2,Ube2G1, UbeU1), HECT E3 (SMURF 2, UbcH7), or RING E3 (Rnf168) tested. CC0651 is shown to target Ub-bound Cdc34 with a 14-fold higher affinity than the non-Ub-bound Cdc34 via an allosteric binding pocket at the periphery of the Cdc34-Ub interface. In addition to inhibit the reactivity of the Cdc34-Ub complex via direct binding, the CC0651-bound Cdc34-Ub complex itself is reported to exhibit higher affinity toward SCF E3 complex and thereby exhibit a dominant negative effect by effectively competing against functional Cdc34-Ub complex for SCF binding. |
Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Primary Target E2 ubiquitin-conjugating enzyme Cdc34 Reversible: yes |
Warning【警告】 | Toxicity: Standard Handling (A) |
Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. |
Other Notes【其他说明】 | Huang, H., et al. 2013. Nat. Chem. Biol.10, 156. Ceccarelli, D.F., et al. 2011. Cell145, 1075. |
Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥98% (HPLC) |
form【形式】 | powder |
optical purity【光学纯度】 | ee: ≥98% |
manufacturer/tradename | Calbiochem® |
storage condition【储存条件】 | OK to freeze protect from light |
color【颜色】 | off-white |
solubility【溶解性】 | DMSO: 100 mg/mL |
storage temp.【储存温度】 | −20℃ |
packaging【包装】 | Packaged under inert gas |
安全信息
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 3 |