Capzimin
Based on 5 publication(s) in Google Scholar
Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.04%
- CAS 番号: 2084868-04-0
- 分子式: C30H24N6O2S4
- 分子量:628.81
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Histological Imaging/Staining
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IF
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IHC
生物活性
Target: Rpn11[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
3.8 μM
Compound: 35
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Antiproliferative activity against human A549 cells after 72 hrs by Cell Titer-Glo assay
Antiproliferative activity against human A549 cells after 72 hrs by Cell Titer-Glo assay
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[PMID: 28191850] |
| HEK-293T | IC50 |
2.1 μM
Compound: 35
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Antiproliferative activity against human 293T cells after 72 hrs by Cell Titer-Glo assay
Antiproliferative activity against human 293T cells after 72 hrs by Cell Titer-Glo assay
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[PMID: 28191850] |
| HeLa | IC50 |
0.6 μM
Compound: 35
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Inhibition of 26S proteasome regulatory subunit RPN11 deubiquitinating activity in beta5 inhibitor MG132 pretreated human HeLa cells expressing UbG76V-GFP assessed as reduction in UbG76V-GFP degradation rate by fluorescence microscopic method
Inhibition of 26S proteasome regulatory subunit RPN11 deubiquitinating activity in beta5 inhibitor MG132 pretreated human HeLa cells expressing UbG76V-GFP assessed as reduction in UbG76V-GFP degradation rate by fluorescence microscopic method
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[PMID: 28191850] |
Capzimin (3027) shows 80-fold selectivity for Rpn11 over Csn5, 10-fold over AMSH and 6-fold over BRCC36 (IC50=30 μM, 4.5 μM and 2.3 μM respectively. Capzimin is screened against the NCI panel of 60 cancer cell lines. The median GI50 is 3.3 μM. Capzimin exhibits promising activity in leukemia cells including the SR and K562 cell lines (GI50 values of 0.67 μM and 1 μM respectively), as well as several solid tumor cell lines including NCI-H460 (non-small cell lung cancer; GI50= 0.7 μM) and MCF7 (breast cancer; GI50=1.0 μM). Immunoblotting for the processed form of caspase 3 and caspase-cleaved poly ADP-ribose polymerase in HCT116 cells confirm that Capzimin not only blocks cell growth, but also induces apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2084868-04-0
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性状 Solid
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分子量 628.81
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分子式 C30H24N6O2S4
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Color White to yellow
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SMILES
O=C(C1=CC2=CC=CC(SSC3=C4N=CC(C(NCCC5=NC=CS5)=O)=CC4=CC=C3)=C2N=C1)NCCC6=NC=CS6
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Sci Immunol
Pharmacological targeting of NLRP3 deubiquitination for treatment of NLRP3-associated inflammatory diseases. [Abstract]2021 Apr 30;6(58):eabe2933. PMID: 33931568 -
Nat Commun
The adaptor protein AP-3β disassembles heat-induced stress granules via 19S regulatory particle in Arabidopsis. [Abstract]2025 Feb 27;16(1):2039. PMID: 40016204 -
Cancer Lett
POH1 facilitates pancreatic carcinogenesis through MYC-driven acinar-to-ductal metaplasia and is a potential therapeutic target. [Abstract]2023 Nov 28:577:216444. PMID: 37844756
Capzimin purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2023 Nov 28:577:216444. [Abstract]
Intraperitoneal injection of Capzimin (10 mg/kg twice a week for 5 weeks) in Pdx1-Cre+;KrasG12D;Trp53R172H+ (KPC) mice leads to reduced neoplastic areas in pancreatic tissue, as determined by H&E staining.
Capzimin purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2023 Nov 28:577:216444. [Abstract]
Capzimin (10 mg/kg) treatment reduces the expression of CK19 in pancreatic tissues of KPC mice, as shown by immunofluorescent staining.
Capzimin purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2023 Nov 28:577:216444. [Abstract]
Capzimin (10 mg/kg) treatment leads to reduced expression of MYC protein in pancreatic tissues of KPC mice, as shown by immunohistochemical analyses.
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J Transl Med
Doxorubicin synergizes bortezomib-induced multiple myeloma cell death by inhibiting aggresome formation and augmenting endoplasmic reticulum/Golgi stress and apoptosis. [Abstract]2024 Dec 3;22(1):1095. PMID: 39623468
Capzimin purchased from MedChemExpress. Usage Cited in: J Transl Med. 2024 Dec 3;22(1):1095. [Abstract]
Capzimin does not stimulate aggresome formation. U266B1 cells treated with no compound or 5 μΜ Capzimin for 24 h, which resulted in ~ 30% cell death, were analyzed for aggresome formation using immunofluorescence.
Capzimin purchased from MedChemExpress. Usage Cited in: J Transl Med. 2024 Dec 3;22(1):1095. [Abstract]
Capzimin does not synergize with Doxorubicin to enhance cell death. U266B1 cells treated with no chemical, 5 μΜ Capzimin, or Capzimin plus 1 μΜ doxorubicin for 24 h were analyzed for cell death using the trypan blue exclusion assay.
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Prostate
Targeting POH1 inhibits prostate cancer cell growth and enhances the suppressive efficacy of androgen deprivation and docetaxel. [Abstract]2019 Aug;79(11):1304-1315. PMID: 31212367
Capzimin purchased from MedChemExpress. Usage Cited in: Prostate. 2019 Aug;79(11):1304-1315. [Abstract]
22RV1 and PC3 cells are treated with or without Capzimin (5 μM) for 48 hours, and the indicated proteins are detected by Western blot analysis.
溶剤 & 溶解度
DMSO : ≥ 55.67 mg/mL (88.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
Fluorescence polarization assays are performed in low-volume 384 well solid black plates in quadruplicate. The assays are performed in buffer containing 50 mM Tris-HCl pH7.5, 1mM MgCl2, 50 μM ATP, 1 mM DTT and 0.01% NP-40. The components for the assay are added in the follow sequence: 1) 5 μL compound (Capzimin, et al.) (in 3% DMSO) at different concentrations, 2) 5 μL of diluted human 26S proteasome, and 3) 5μL of substrate (3 nM Ub4- peptideOG). 100 μM Zn(cyclen)2+ is present in the titration reaction for the experiments performed with Zn(cyclen)2+. Fluorescence polarization is measured at 30°C with excitation at 480 nm and emission at 520 nm. Collected data is normalized to DMSO control and fitted to a dose-response curve to determine the IC50 value[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
HCT116 cells are treated with different concentrations of 3021 or Capzimin for 72 hours in normal or low serum medium and then mixed with CellTiter-Glo reagent to estimate cell proliferation. Measured luminescence values are normalized to DMSO control and data are fitted to a dose-response equation to determine the GI50[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5903 mL | 7.9515 mL | 15.9031 mL | 39.7576 mL |
| 5 mM | 0.3181 mL | 1.5903 mL | 3.1806 mL | 7.9515 mL | |
| 10 mM | 0.1590 mL | 0.7952 mL | 1.5903 mL | 3.9758 mL | |
| 15 mM | 0.1060 mL | 0.5301 mL | 1.0602 mL | 2.6505 mL | |
| 20 mM | 0.0795 mL | 0.3976 mL | 0.7952 mL | 1.9879 mL | |
| 25 mM | 0.0636 mL | 0.3181 mL | 0.6361 mL | 1.5903 mL | |
| 30 mM | 0.0530 mL | 0.2651 mL | 0.5301 mL | 1.3253 mL | |
| 40 mM | 0.0398 mL | 0.1988 mL | 0.3976 mL | 0.9939 mL | |
| 50 mM | 0.0318 mL | 0.1590 mL | 0.3181 mL | 0.7952 mL | |
| 60 mM | 0.0265 mL | 0.1325 mL | 0.2651 mL | 0.6626 mL | |
| 80 mM | 0.0199 mL | 0.0994 mL | 0.1988 mL | 0.4970 mL |
Capzimin 関連分類
HY-110404 関連分類
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