PROTAC Bcl-xL degrader-4
PROTAC Bcl-xL degrader-4 is a Bcl-xL PROTAC degrader. PROTAC Bcl-xL degrader-4 exhibits cytotoxicity against hepatocellular carcinoma cells, inhibits their migration and colony formation, and shows low cytotoxicity toward normal cells. PROTAC Bcl-xL degrader-4 induces apoptosis by reducing mitochondrial membrane potential and activating the MAPK signaling pathway. PROTAC Bcl-xL degrader-4 significantly suppresses tumor growth in xenograft tumor mouse models. PROTAC Bcl-xL degrader-4 can be used in hepatocellular carcinoma-related research.
(Pink: Bcl-xL ligand (HY-176741); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W017440)).
For research use only. We do not sell to patients.
- CAS No.: 2930759-37-6
- Formula: C39H34N4O9
- Molecular Weight:702.71
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Biological Activity
Description
IC50 & Target
[1]|
Bcl-2 |
Bcl-xL |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
3.50 μM
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Cytotoxicity against human HepG2 hepatocellular carcinoma cells assessed as reduction in cell viability by MTT assay.
Cytotoxicity against human HepG2 hepatocellular carcinoma cells assessed as reduction in cell viability by MTT assay.
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40517590 |
| HUVEC | IC50 |
58.63 μM
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Cytotoxicity against human HUVEC umbilical vein endothelial cells assessed as reduction in cell viability by MTT assay.
Cytotoxicity against human HUVEC umbilical vein endothelial cells assessed as reduction in cell viability by MTT assay.
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40517590 |
In Vitro
PROTAC Bcl-xL degrader-4 (Compound 2-38-III) potently inhibits the viability of HepG2 cells with an IC50 of 3.50 μM; meanwhile, it shows low cytotoxicity against HUVEC cells with an IC50 of 58.63 μM[1].
PROTAC Bcl-xL degrader-4 (3 μM; 10 days) potently inhibits colony formation of HepG2 cells[1].
PROTAC Bcl-xL degrader-4 (3 μM; 48 h) potently inhibits lateral migration of HepG2 cells[1].
PROTAC Bcl-xL degrader-4 (1 μM; 24 h) potently inhibits the longitudinal migration of HepG2 cells[1].
PROTAC Bcl-xL degrader-4 (1 μM; 12 h) potently inhibits tube formation in HUVEC cells, thereby suppressing neovascularization[1].
PROTAC Bcl-xL degrader-4 (1-3 μM; 48 h) activates the MAPK pathway in HepG2 cells by upregulating the expression of P-ERK, P-p38 and P-JNK[1].
PROTAC Bcl-xL degrader-4 (3-10 μM; 24-48 h) induces apoptosis in HepG2 cells[1].
PROTAC Bcl-xL degrader-4 (0.3-3 μM; 48 h) regulates mitochondrial apoptosis pathway proteins in HepG2 cells by downregulating Bcl-xL and Bcl-2, upregulating Bax, and increasing the expression of cytochrome C[1].
PROTAC Bcl-xL degrader-4 (3-10 μM; 24-48 h) reduces the mitochondrial membrane potential of HepG2 cells in a dose- and time-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 human hepatocellular carcinoma cells
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Concentration:3 μM
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Incubation Time:10 days
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Result:Markedly reduced colony number relative to DMSO, sorafenib, and 2-38 groups, resulting in the lowest colony formation rate.
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Cell Line:HepG2 human hepatocellular carcinoma cells
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Concentration:3 μM
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Incubation Time:48 h (measured at 12 h, 24 h, 36 h, 48 h time points)
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Result:Significantly reduced migration distance of HepG2 cells compared to control and other treatment groups.
Resulted in minimal wound closure observed by 48 h.
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Cell Line:HepG2 human hepatocellular carcinoma cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Markedly reduced the number of migrated HepG2 cells compared to control and other treatment groups.
Achieved the lowest count of migrated cells among all tested compounds.
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Cell Line:HepG2 human hepatocellular carcinoma cells
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Concentration:3 μM, 10 μM
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Incubation Time:24 h, 48 h
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Result:Induced apoptosis in HepG2 cells, with an apoptosis rate of 12.4% at 3 μM for 24 h.
Induced apoptosis in HepG2 cells, with an apoptosis rate of 36.6% at 10 μM for 24 h.
Induced apoptosis in HepG2 cells, with an apoptosis rate of 43.3% at 3 μM for 48 h.
Induced apoptosis in HepG2 cells, with an apoptosis rate of 45.4% at 10 μM for 48 h.
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Cell Line:HepG2 human hepatocellular carcinoma cells
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Concentration:0.3 μM, 1 μM, 3 μM
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Incubation Time:48 h
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Result:Dose-dependently down-regulated expression of anti-apoptotic proteins Bcl-xL and Bcl-2 relative to control.
Dose-dependently up-regulated expression of pro-apoptotic protein Bax relative to control.
Dose-dependently increased expression of cytochrome C relative to control.
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Cell Line:HepG2 human hepatocellular carcinoma cells
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Concentration:1 μM, 3 μM
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Incubation Time:48 h
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Result:Up-regulated expression of phosphorylated ERK (P-ERK) in HepG2 cells relative to control.
Up-regulated expression of phosphorylated p38 (P-p38) in HepG2 cells relative to control.
Up-regulated expression of phosphorylated JNK (P-JNK) in HepG2 cells relative to control.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (6 mice per group)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; every other day; 18 days
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Result:Maintained stable mouse body weights with no significant changes in serum AST, ALP, or BUN levels.
Achieved a tumor inhibition rate of 30.94% at 10 mg/kg.
Achieved a tumor inhibition rate of 58.48% at 20 mg/kg.
Confirmed suppression of tumor cell proliferation via H&E staining.
Inhibited tumor cell proliferation, metastasis, and vascular neovascularization via immunofluorescence analysis of Ki-67 and CD31.
Chemical Information
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CAS No. 2930759-37-6
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Molecular Weight 702.71
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Formula C39H34N4O9
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SMILES
O=C1N(C(C2=CC=CC(NCCOCCOCCOC(C3=CC4=C(NC(C5=CC=CC6=C5C=CC=C6)=CC4=O)C=C3)=O)=C21)=O)C7CCC(NC7=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC Bcl-xL degrader-4 Related Classifications
HY-176740 Related Classifications
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Keywords
- PROTAC Bcl-xL degrader-4
- 2930759-37-6
- PROTACs
- p38 MAPK
- Mitochondrial Metabolism
- Reactive Oxygen Species (ROS)
- Apoptosis
- Bcl-2 Family
- ERK
- JNK
- hepatocellular carcinoma
- BALB/c nude mice
- endothelial cells
- MAPK pathways
- HUVEC cells
- apoptosis
- neovascularization
- HepG2 cells
- mitochondrial pathways
- cytochrome C
- Inhibitor
- inhibitor
- inhibit