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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.66%
- No. CAS: 518303-20-3
- Fòrmula: C18H14BrNO5S2
- Peso molecular:468.34
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Almacenamiento: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
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) UMI-77
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Customer Validation & Images
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WB
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Cell Imaging/Staining
Actividad biológica
Descripciòn
IC50 & Target
[1]|
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) |
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 518303-20-3
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Appearance Solid
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Peso molecular 468.34
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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Solvente y solubilidad
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
In Vivo Dissolution Calculator
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.
Protocolo
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Pureza y Documentación
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Ficha de datos (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- 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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Instrucciones de manejo (2659 KB)
Referencias
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 Related Classifications
HY-18628 Related Classifications
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