MDK83190
Based on 1 Customer Validation
MDK83190 is a potent apoptosis activator, induces Apaf-1 oligomerization, increases procaspase-9 processing and subsequent caspase-3 activation in a cyto c-dependent Manner.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.61%
- No. CAS: 79183-19-0
- Fòrmula: C15H9Cl2NO2
- Peso molecular:306.14
-
Almacenamiento: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]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
HY-13523
PAC-1Caspase Activator -
HY-16658B
Z-VAD-FMKPan-Caspase Inhibitor -
HY-12305
Q-VD-OPhPan-caspase Inhibitor -
HY-16658
Z-VAD(OMe)-FMKPan-caspase Inhibitor -
HY-13205
BelnacasanCaspase-1 Inhibitor -
HY-12466
Z-DEVD-FMKCaspase-3 Inhibitor -
HY-10396
Emricasanpan-Caspase Inhibitor -
HY-N0087
Gambogic AcidBcl-2 Family Inhibitor -
HY-101297
Z-IETD-FMKCaspase-8 Inhibitor -
HY-13229
BOC-D-FMKCaspase Inhibitor -
HY-P1010
Z-LEHD-FMKCaspase-9 Inhibitor -
HY-13721
PhenoxodiolAnticancer Agent
Actividad biológica
Descripciòn
IC50 & Target
IC50: 4-9 uM (Leukemia origin cells)[1].
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
>50 μM
Compound: 1
|
Antiproliferative activity against human HCT-116p53KO subline assessed as growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116p53KO subline assessed as growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34902732] |
| HCT-116 | IC50 |
38 μM
Compound: 1
|
Antiproliferative activity against human HCT-116 assessed as growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 assessed as growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34902732] |
| K562 | IC50 |
20 μM
Compound: 1
|
Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34902732] |
| MCF7 | IC50 |
>50 μM
Compound: 1
|
Antiproliferative activity against human MCF7 cells assessed as growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34902732] |
| MCF7 | IC50 |
>50 μM
Compound: 1
|
Antiproliferative activity against human MCF7 cells assessed as growth inhibition under hypoxia conditions measured after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as growth inhibition under hypoxia conditions measured after 72 hrs by MTT assay
|
[PMID: 34902732] |
| MDA-MB-231 | IC50 |
>50 μM
Compound: 1
|
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition under hypoxia conditions measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition under hypoxia conditions measured after 72 hrs by MTT assay
|
[PMID: 34902732] |
| MDA-MB-231 | IC50 |
>50 μM
Compound: 1
|
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition under normoxia conditions measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition under normoxia conditions measured after 72 hrs by MTT assay
|
[PMID: 34902732] |
In Vitro
MDK83190 (Compound 2) (1-50 μM; 2 hours) effects against cell lines of lymphoid origin (CCRF-CEM, MOLT-4, and Jurkat) with IC50 values ranging from 4 to 9 μM[1]. MDK83190 (Compound 2) (20 μM; 30 mins) activates procaspase-9 and procaspase-3 in a cyto c-dependent manner[1]. MDK83190 (Compound 2) (0.1-100 μM; 22 hours) strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation, and finally killing cells with an IC50 of 4 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:Leukemia cell line: CCRF-CEM cells, MOLT-4 cells, and Jurkat cells
-
Concentration:1-50 μM
-
Incubation Time:2 hours
-
Result:Was sensitive to compound 2-induced apoptosis.
-
Cell Line:Hela cells
-
Concentration:20 μM
-
Incubation Time:30 mins
-
Result:Induced procaspase-9 and procaspase-3 to active forms.
-
Cell Line:Jurkat cells
-
Concentration:0.1-100 μM
-
Incubation Time:22 hours
-
Result:Resulted in apoptosis and finally killed cells.
Chemical Information
-
No. CAS 79183-19-0
-
Appearance Solid
-
Peso molecular 306.14
-
Fòrmula C15H9Cl2NO2
-
Color Yellow to orange
-
SMILES
O=C1N(CC2=CC=C(Cl)C(Cl)=C2)C3=C(C=CC=C3)C1=O
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
In Vitro:
DMSO : ≥ 46 mg/mL (150.26 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.
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 (8.17 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
-
TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
-
Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
-
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
-
Ficha de datos (278 KB)
-
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)
-
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, 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 | 3.2665 mL | 16.3324 mL | 32.6648 mL | 81.6620 mL |
| 5 mM | 0.6533 mL | 3.2665 mL | 6.5330 mL | 16.3324 mL | |
| 10 mM | 0.3266 mL | 1.6332 mL | 3.2665 mL | 8.1662 mL | |
| 15 mM | 0.2178 mL | 1.0888 mL | 2.1777 mL | 5.4441 mL | |
| 20 mM | 0.1633 mL | 0.8166 mL | 1.6332 mL | 4.0831 mL | |
| 25 mM | 0.1307 mL | 0.6533 mL | 1.3066 mL | 3.2665 mL | |
| 30 mM | 0.1089 mL | 0.5444 mL | 1.0888 mL | 2.7221 mL | |
| 40 mM | 0.0817 mL | 0.4083 mL | 0.8166 mL | 2.0415 mL | |
| 50 mM | 0.0653 mL | 0.3266 mL | 0.6533 mL | 1.6332 mL | |
| 60 mM | 0.0544 mL | 0.2722 mL | 0.5444 mL | 1.3610 mL | |
| 80 mM | 0.0408 mL | 0.2042 mL | 0.4083 mL | 1.0208 mL | |
| 100 mM | 0.0327 mL | 0.1633 mL | 0.3266 mL | 0.8166 mL |
MDK83190 Related Classifications
HY-18633 Related Classifications
Powered by Bioz