dMCL1-2
Based on 1 Customer Validation
dMCL1-2 is a potent, selective MCL1 PROTAC degrader based on a Cereblon ligand, with a KD value of 30 nM for binding to MCL1. dMCL1-2 induces ubiquitination and degradation of MCL1. dMCL1-2 degrades MCL1, cleaves Caspase-3, and induces Apoptosis. dMCL1-2 can be used in research related to multiple myeloma.
(Pink: MCL1 ligand (HY-125908); Blue: Cereblon ligand (HY-103596); Black: linker).
For research use only. We do not sell to patients.
- Purity : 99.29%
- CAS No.: 2351218-88-5
- Formula: C61H66N10O12S
- Molecular Weight:1163.30
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
MCL1 30 nM (Kd) |
Caspase 3 |
In Vitro
dMCL1-2 (50-500 nM; 24 h) induces apoptosis in OPM2 multiple myeloma cells following 24-hour incubation in medium containing 1% FBS[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:OPM2 multiple myeloma cells
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Concentration:50; 100; 250; 500 nM
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Incubation Time:24 h
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Result:Increased cleaved caspase-3 abundance to 197% of the DMSO control at 250 nM.
Increased cleaved caspase-3 abundance to 326% of the DMSO control at 500 nM.
Reduced MCL1-long abundance to 73% and 55% of the control, and MCL1-short abundance to 49% and 22% of the control for 250 nM and 500 nM, respectively.
Chemical Information
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CAS No. 2351218-88-5
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Appearance Solid
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Molecular Weight 1163.30
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Formula C61H66N10O12S
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Color White to off-white
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SMILES
O=S(N(CC1)CCN1C(C=C2)=CC=C2OCC3=C(C4=C(N(CCN5CCN(C(COC6=CC=CC(C(N7C8C(NC(CC8)=O)=O)=O)=C6C7=O)=O)CC5)C(C(O)=O)=C9CCCOC%10=C(C=CC=C%11)C%11=CC=C%10)C9=CC=C4)C(C)=NN3C)(N(C)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (85.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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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.
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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.
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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
Purity & Documentation
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Data Sheet (275 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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Handling Instructions (2659 KB)
References
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 |
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| DMSO | 1 mM | 0.8596 mL | 4.2981 mL | 8.5962 mL | 21.4906 mL |
| 5 mM | 0.1719 mL | 0.8596 mL | 1.7192 mL | 4.2981 mL | |
| 10 mM | 0.0860 mL | 0.4298 mL | 0.8596 mL | 2.1491 mL | |
| 15 mM | 0.0573 mL | 0.2865 mL | 0.5731 mL | 1.4327 mL | |
| 20 mM | 0.0430 mL | 0.2149 mL | 0.4298 mL | 1.0745 mL | |
| 25 mM | 0.0344 mL | 0.1719 mL | 0.3438 mL | 0.8596 mL | |
| 30 mM | 0.0287 mL | 0.1433 mL | 0.2865 mL | 0.7164 mL | |
| 40 mM | 0.0215 mL | 0.1075 mL | 0.2149 mL | 0.5373 mL | |
| 50 mM | 0.0172 mL | 0.0860 mL | 0.1719 mL | 0.4298 mL | |
| 60 mM | 0.0143 mL | 0.0716 mL | 0.1433 mL | 0.3582 mL | |
| 80 mM | 0.0107 mL | 0.0537 mL | 0.1075 mL | 0.2686 mL |
dMCL1-2 Related Classifications
HY-128360 Related Classifications
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