PROTAC Bcl-xL degrader-2
Based on 1 Customer Validation
PROTAC Bcl-xL degrader-2 is a selective Bcl-xL PROTAC degrader with a DC50 of 4.8 nM against Bcl-xL. PROTAC Bcl-xL degrader-2 forms a ternary complex with VHL E3 ligase, thereby redirecting the ubiquitin-proteasome system to mediate the degradation of Bcl-xL. PROTAC Bcl-xL degrader-2 triggers Apoptosis. PROTAC Bcl-xL degrader-2 can be used in the research of solid tumors and hematologic malignancies.
(Pink: Bcl-xL ligand (HY-184713); Blue: VHL ligand (HY-125845); Black: linker (HY-133051)).
For research use only. We do not sell to patients.
- Purity: 98.23%
- CAS No.: 2920415-08-1
- Formula: C68H80N8O14S3
- Molecular Weight:1329.60
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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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
Bcl-xL 4.8 nM (DC50) |
VHL |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | DC50 |
4.8 nM
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Induction of Bcl-xL protein degradation in human THP-1 cells assessed by Western blot after 24 h incubation.
Induction of Bcl-xL protein degradation in human THP-1 cells assessed by Western blot after 24 h incubation.
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32697072 |
In Vitro
PROTAC Bcl-xL degrader-2 (Compound 6) potently binds purified Bcl-xL protein with an IC50 of 0.6 nM in a HTRF ligand displacement assay[1].
PROTAC Bcl-xL degrader-2 (0.1-3000 nM; 24 h) induces degradation of Bcl-xL in THP-1 cells with a DC50 of 4.8 nM and 76% maximum degradation after 24 h incubation, exhibiting a hook effect at concentrations above 300 nM[1].
PROTAC Bcl-xL degrader-2 forms a 1.9 Å resolution ternary complex with VCB and Bcl-xL proteins, featuring a compact folded linker, a 672 Å2 neo-protein/protein interface, and extensive specific intermolecular interactions despite exhibiting modest negative cooperativity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 cells
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Concentration:0.1-~3162 nM
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Incubation Time:24 h
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Result:Caused monotonic decreases in Bcl-xL protein levels with increasing concentrations from 0.1 nM to 300 nM.
Led to a recovery of Bcl-xL levels at concentrations above 300 nM (hook effect).
Achieved a DC50 for Bcl-xL degradation of 4.8 nM, with a maximum degradation (MaxD) of 76% after 24 h.
Chemical Information
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CAS No. 2920415-08-1
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Appearance Solid
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Molecular Weight 1329.60
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Formula C68H80N8O14S3
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Color White to off-white
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SMILES
O=C(C1=C(CCCOC2=CC=C(C#CCOCCOCCOCCOCCOCCOCCC(N[C@H](C(N3[C@H](C(NCC4=CC=C(C5=C(C)N=CS5)C=C4)=O)C[C@@H](O)C3)=O)C(C)(C)C)=O)C=C2)SC(N6CC7=C(C=CC=C7C(NC8=NC9=CC=CC=C9S8)=O)CC6)=N1)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 (75.21 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.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.7521 mL | 3.7605 mL | 7.5211 mL | 18.8026 mL |
| 5 mM | 0.1504 mL | 0.7521 mL | 1.5042 mL | 3.7605 mL | |
| 10 mM | 0.0752 mL | 0.3761 mL | 0.7521 mL | 1.8803 mL | |
| 15 mM | 0.0501 mL | 0.2507 mL | 0.5014 mL | 1.2535 mL | |
| 20 mM | 0.0376 mL | 0.1880 mL | 0.3761 mL | 0.9401 mL | |
| 25 mM | 0.0301 mL | 0.1504 mL | 0.3008 mL | 0.7521 mL | |
| 30 mM | 0.0251 mL | 0.1254 mL | 0.2507 mL | 0.6268 mL | |
| 40 mM | 0.0188 mL | 0.0940 mL | 0.1880 mL | 0.4701 mL | |
| 50 mM | 0.0150 mL | 0.0752 mL | 0.1504 mL | 0.3761 mL | |
| 60 mM | 0.0125 mL | 0.0627 mL | 0.1254 mL | 0.3134 mL |
PROTAC Bcl-xL degrader-2 Related Classifications
HY-139309 Related Classifications
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