UMI-77
Based on 5 publication(s) in Google Scholar
UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
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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: 99.66%
- CAS 番号: 518303-20-3
- 分子式: C18H14BrNO5S2
- 分子量:468.34
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 UMI-77
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WB
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Cell Imaging/Staining
生物活性
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Mcl-1 0.49 μM (Ki) |
Bfl-1 5.33 μM (Ki) |
Bcl-W 8.19 μM (Ki) |
Bcl-2 23.83 μM (Ki) |
Bcl-xL 32.99 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
11.37 μM
Compound: UMI-77
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Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay
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[PMID: 32088497] |
| HL-60 | IC50 |
3.13 μM
Compound: 10
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Cytotoxicity against human HL60 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay
Cytotoxicity against human HL60 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay
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[PMID: 24749893] |
| Jurkat | IC50 |
9.79 μM
Compound: UMI-77
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Antiproliferative activity against human Jurkat cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human Jurkat cells incubated for 72 hrs by MTT assay
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[PMID: 32088497] |
| K562 | IC50 |
15.11 μM
Compound: 10
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Cytotoxicity against human K562 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay
Cytotoxicity against human K562 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay
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[PMID: 24749893] |
| MOLT-4 | IC50 |
3.14 μM
Compound: UMI-77
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Antiproliferative activity against human MOLT-4 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human MOLT-4 cells incubated for 72 hrs by MTT assay
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[PMID: 32088497] |
| MV4-11 | IC50 |
10.87 μM
Compound: 10
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Cytotoxicity against human MV4-11 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay
Cytotoxicity against human MV4-11 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay
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[PMID: 24749893] |
| NCI-H1299 | IC50 |
6.08 μM
Compound: UMI-77
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Antiproliferative activity against human NCI-H1299 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1299 cells incubated for 72 hrs by MTT assay
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[PMID: 32088497] |
| PC-3 | IC50 |
8.43 μM
Compound: UMI-77
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Antiproliferative activity against human PC-3 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells incubated for 72 hrs by MTT assay
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[PMID: 32088497] |
| RPMI-8226 | IC50 |
5.77 μM
Compound: UMI-77
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Antiproliferative activity against human RPMI-8226 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human RPMI-8226 cells incubated for 72 hrs by MTT assay
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[PMID: 32088497] |
Competitive binding curve of UMI-77 against Mcl-1 is obtained by FP based binding assay using fluorescent labeled Bid BH3 peptide with an IC50 of 1.87±0.22 μM. UMI-77 potently inhibits the cell growth of BxPC-3 and Panc-1 cell lines with IC50 values of 3.4 μM and 4.4 μM respectively, and shows 3 to 5 times less potency in inhibition of the cell growth of two other tested cell lines MiaPaCa-2 (12.5 μM) and AsPC-1 (16.1 μM). The cell growth inhibition potency of UMI-77 correlates with the highest expression of Mcl-1 and Bak, and lowest expression of Bcl-xL in the sensitive cell lines, BxPC-3 and Panc-1. Capan-2 cells are showing similar sensitivity to UMI-77 (IC50 of 5.5 μM) as BxPC-3 and Panc-1, although has low Mcl-1 levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 518303-20-3
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性状 Solid
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分子量 468.34
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分子式 C18H14BrNO5S2
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Color White to off-white
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SMILES
O=C(O)CSC1=CC(NS(=O)(C2=CC=C(Br)C=C2)=O)=C3C=CC=CC3=C1O
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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 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell Death Differ
2026 May 7. PMID: 42098326 -
Cancer Cell Int
2022 Oct 7;22(1):304. PMID: 36207761
UMI-77 purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2022 Oct 7;22(1):304. [Abstract]
UMI-77 (10 μM, 24 h) activated the expression of mitophagyrelated proteins suppressed by cirsiliol, including PINK1, Parkin, BNIP3, and FUNDC1 by western blot analysis.
UMI-77 purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2022 Oct 7;22(1):304. [Abstract]
UMI-77 (10 μM) relieved ∆Ψm loss caused by cirsiliol. Representative images of JC-1 staining.
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CNS Neurosci Ther
Hippocampal mitophagy contributes to spatial memory via maintaining neurogenesis during the development of mice. [Abstract]2024 Jun;30(6):e14800. PMID: 38887162 -
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溶剤 & 溶解度
DMSO : ≥ 28 mg/mL (59.79 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (5.34 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.34 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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
Human PC cell lines AsPC-1, BxPC-3 and Capan-2 are cultured in RPMI 1640 medium, while Panc-1 and MiaPaCa are cultured in DMEM medium, all supplemented with 10% fetal bovine serum. The cell growth inhibition after treatment with increasing concentrations of the compounds (e.g., UMI-77; 1,10, and 100 μM) is determined by WST-8 assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
For BxPC-3 subcutaneous model, 10×106 cells are subcutaneously injected into the flanks of 4-5 week old female severe combined immune deficient mice (ICR-SCID). Palpable tumors start to appear in 3-5 weeks. Tumors are measured twice weekly. To prevent any pain or discomfort, mice are euthanized and their tumors remove once they reach ~1800 mg burden. Tumors are then dissected into 50 mg pieces and re-transplanted into naïve ICR-SCID for serial propagation. Animals are treated with either vehicle or UMI-77 given i.v. (60 mg/kg) on day three post BxPC-3 transplantation for two weeks (5 days a week). Tumor weight is recorded throughout the treatment period. At the end of the treatment period, animals are euthanized and their tumors harvested for protein isolation and western blot analysis for apoptotic markers.
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 (285 KB)
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SDS (393 KB)
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- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1352 mL | 10.6760 mL | 21.3520 mL | 53.3800 mL |
| 5 mM | 0.4270 mL | 2.1352 mL | 4.2704 mL | 10.6760 mL | |
| 10 mM | 0.2135 mL | 1.0676 mL | 2.1352 mL | 5.3380 mL | |
| 15 mM | 0.1423 mL | 0.7117 mL | 1.4235 mL | 3.5587 mL | |
| 20 mM | 0.1068 mL | 0.5338 mL | 1.0676 mL | 2.6690 mL | |
| 25 mM | 0.0854 mL | 0.4270 mL | 0.8541 mL | 2.1352 mL | |
| 30 mM | 0.0712 mL | 0.3559 mL | 0.7117 mL | 1.7793 mL | |
| 40 mM | 0.0534 mL | 0.2669 mL | 0.5338 mL | 1.3345 mL | |
| 50 mM | 0.0427 mL | 0.2135 mL | 0.4270 mL | 1.0676 mL |
UMI-77 関連分類
HY-18628 関連分類
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