1. Metabolic Enzyme/Protease
  2. E1/E2/E3 Enzyme
  3. CC0651

CC0651 是一种人Cdc34泛素结合酶变构抑制剂。CC0651 有效抑制 p27Kip1的泛素化,IC50 为 1.72 μM。

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CC0651 Chemical Structure

CC0651 Chemical Structure

CAS No. : 1319207-44-7

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1 mg ¥5115
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5 mg ¥9114
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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27Kip1, as confirmed by dose-response analysis.

IC50 & Target

IC50: 1.72 μM (p27Kip1 ubiquitination)[1]

体外研究
(In Vitro)

CC0651 strongly impairs the rate of ubiquitin chain initiation on substrate by SCFCdc4, as measured by the monoubiquitination of Sic1 by K0 ubiquitin. CC0651 actually potentiates the formation of both ubiquitin dimers and monoubiquitinated hCdc34, concordant with the observed accumulation of the hCdc34 conjugate in cells treated with the ester derivative of CC0651. CC0651 completely inhibits the assembly of polyubiquitin chains and decreased formation of free triubiquitin and, to a lesser extent, hCdc34 monoubiquitin, but has no effect on production of diubiquitin[1]. CC0651 is an inhibitor of the E2 ubiquitin conjugating enzyme Cdc34A, acts by trapping a weak interaction between ubiquitin and the E2 donor ubiquitin binding site. A quantitative SCF ubiquitination assay with a β-Catenin substrate peptide yields a value of IC50 of 18±1 μM for CC0651 inhibition, similar to the effective concentrations observed in the NMR and TR-FRET assays[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

442.29

Formula

C20H21Cl2NO6

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 56 mg/mL (126.61 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2610 mL 11.3048 mL 22.6096 mL
5 mM 0.4522 mL 2.2610 mL 4.5219 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.03%

参考文献
Kinase Assay
[1]

For small-molecule screens, p27Kip1 is ubiquitinated in a 15 μL reaction with 40 nM phospho-p27, 40 nM E1, 5 μM E2, 25 nM SCFSkp2, 25 nM Cks1, and 27.8 μM biotinylated ubiquitin in 40 mM Tris-HCl [pH 7.5], 5 mM MgCl2, 1 mM DTT, and 0.5 mM ATP at 23°C for 3 hr. The reaction is terminated with assay diluent, transferred to 384-well protein A plates coated with 62 ng SC528 antibody, incubated for 1 hr, and washed six times with 10 mM Tris-HCl [pH 7.6], 0.05% Tween20 prior to addition of 25 μL of 0.4 mg/mL europium streptavidin in HEPES [pH 7.6], 1% BSA, 0.2% Tween20 per well. Plates are incubated for 1 hr, washed, and read for Eu-time-resolved fluorescence after addition of 25 μL enhancement solution. For gel-based ubiquitination assays, CC0651 and its analogs are preincubated at the indicated concentrations with 0.5 μg E1, 1-4 μg hCdc34, and 50 ng SCFCdc4, 100 ng SCFFbw7, 150 ng SCFβTrCP, or 50 ng SCFSkp2 for 10-45 min at 4°C in 20 μL reaction buffer (50 mM HEPES [pH 7.5], 10 mM MgCl2, 2 mM ATP, and 50μM DTT). Reactions are initiated by addition of 1μg ubiquitin and respective SCF substrates (50 ng HisSic1 phosphorylated by Cln2-Cdc28, 50ng cyclin E phosphorylated by Cdk2, 25 ng biotinylated IκBα phosphopeptide [KKERLLDDHDpSGLDpSMKDEE], or 50 ng p27Kip1 phosphorylated by cyclin E-Cdk2), incubated at 30°C for 1-3 hr, and products visualized by immunoblot[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

PC-3 and HCT116 cell lines are grown in DMEM supplemented with Penicillin/Streptomycin, 2 mM glutamine, and 10% fetal bovine serum (FBS). Lentiviral shRNA constructs for human CDC34, UBE2R2, and nontarget control are used. For proliferation assays, PC-3 cultures are seeded at 5000 cells/well in quadruplicate in 24-well plates, grown for 24 hr, and then infected with lentiviral supernatant. For small-molecule inhibition, cells are seeded in quadruplicate at 500 cells/well in 96-well plates, grown for 24 hr, and treated with compound. Proliferation is measured by MTT assay. PC-3 or HCT 116 cultures are synchronized in G0/G1 by serum starvation for 30 hr and then released by addition of 10% serum. For epistasis experiments, PC-3 cells are infected with CDC34 shRNA for 24 hr, followed by addition of inhibitor and assessment of proliferation after 4 days. Anti-Cdc34, anti-p27, anti-α-tubulin, anti-ubiquitin, and anti-cyclin E antibodies are used[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2610 mL 11.3048 mL 22.6096 mL 56.5240 mL
5 mM 0.4522 mL 2.2610 mL 4.5219 mL 11.3048 mL
10 mM 0.2261 mL 1.1305 mL 2.2610 mL 5.6524 mL
15 mM 0.1507 mL 0.7537 mL 1.5073 mL 3.7683 mL
20 mM 0.1130 mL 0.5652 mL 1.1305 mL 2.8262 mL
25 mM 0.0904 mL 0.4522 mL 0.9044 mL 2.2610 mL
30 mM 0.0754 mL 0.3768 mL 0.7537 mL 1.8841 mL
40 mM 0.0565 mL 0.2826 mL 0.5652 mL 1.4131 mL
50 mM 0.0452 mL 0.2261 mL 0.4522 mL 1.1305 mL
60 mM 0.0377 mL 0.1884 mL 0.3768 mL 0.9421 mL
80 mM 0.0283 mL 0.1413 mL 0.2826 mL 0.7065 mL
100 mM 0.0226 mL 0.1130 mL 0.2261 mL 0.5652 mL
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产品名称:
CC0651
目录号:
HY-15301
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