NTLiverTac PDE6D degrader-1
NTLiverTac PDE6D degrader-1 is a PDE6D NTLiverTac degrader with a DC50 of 4.09 μM. NTLiverTac PDE6D degrader-1 is formed by conjugating a PDE6D PROTAC degrader with the NTCP ligand Cholic acid (HY-N0324). NTLiverTac PDE6D degrader-1 triggers the ubiquitin-proteasome system-mediated degradation process by forming a complex with PDE6D and MDM2, inducing proteasome-dependent and NTCP-dependent degradation. NTLiverTac PDE6D degrader-1 inhibits PDE6D-dependent KRAS trafficking and suppresses KRAS-related oncogenic signaling cascades. NTLiverTac PDE6D degrader-1 inhibits the activation of the PI3K/AKT/mTOR signaling pathway and induces cellular Apoptosis. NTLiverTac PDE6D degrader-1 enters cancer cells via NTCP-mediated endocytosis. NTLiverTac PDE6D degrader-1 can be used in the research of hepatoblastoma (MDM2 ligand: (4R,5S)-Nutlin carboxylic acid (HY-128836); NTCP ligand: Cholic acid (HY-N0324); PDE6D ligand: Sorafenib (HY-10201)).
For research use only. We do not sell to patients.
- Formula: C93H113Cl3F3N15O17
- Molecular Weight:1876.34
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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]|
PDE6D 4.09 μM (DC50) |
K-RAS |
MDM2 |
In Vitro
NTLiverTac PDE6D degrader-1 (Compound S2C2M2) inhibits the proliferation of HuH-6 cells with an IC50 value of 7.46 μM[1].
NTLiverTac PDE6D degrader-1 (0.3-30 μM; 24-72 h) induces proteasome-dependent and NTCP-dependent degradation of PDE6D in HuH-6 cells, with a DC50 of 4.09 μM at 60 h[1].
NTLiverTac PDE6D degrader-1 (30 μM) inhibits the activation of KRAS in HuH-6 cells[1].
NTLiverTac PDE6D degrader-1 (3.75-30 μM) inhibits EGF-induced activation of the PI3K/AKT/mTOR signaling pathway in HuH-6 cells in a concentration-dependent manner[1].
NTLiverTac PDE6D degrader-1 (7.5-30 μM) induces apoptosis in HuH-6 cells in a concentration-dependent manner by regulating the levels of pro-apoptotic and anti-apoptotic proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human hepatoblastoma HuH-6 cells
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Concentration:0.3-30 μM (PDE6D degradation concentration-dependence); 30 μM (PDE6D degradation time-dependence); 30 μM (pre-treatment with 50 nM proteasome inhibitor MG132, 0.5 μM neddylation inhibitor MLN4924, 30 μM MDM2 ligand Nutlin 3a, 30 μM multikinase inhibitor sorafenib, 10 μM cholic acid, or 0.5 μM NTCP inhibitor bluevirtide)
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Incubation Time:60 h (PDE6D degradation concentration-dependence); 24-72 h (PDE6D degradation time-dependence); 60 h (pre-treatment with inhibitors, with 4 h pre-treatment)
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Result:Induced concentration-dependent PDE6D degradation, with a DC50 (60 h) of 4.09 μM, and reduced PDE6D protein levels by approximately 70% at 30 μM after 72 h.
Induced time-dependent PDE6D degradation, with decreasing protein levels over 72 h at 30 μM.
Blocked KRAS IN-44-mediated PDE6D degradation when cells were pre-treated with proteasome inhibitor MG132, neddylation inhibitor MLN4924, MDM2 ligand Nutlin 3a, multikinase inhibitor sorafenib, NTCP substrate cholic acid, or NTCP inhibitor bluevirtide.
Chemical Information
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Molecular Weight 1876.34
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Formula C93H113Cl3F3N15O17
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SMILES
ClC1=CC=C([C@@H]2[C@H](C3=CC=C(Cl)C=C3)N(C(N4CC(N(CC(NCCOCCOCCN5C=C(COCC(NC(CCNC(CC[C@@H](C)[C@]6([H])[C@]([C@@H](O)C[C@@]7([H])[C@@]8([H])[C@H](O)C[C@@]9([H])[C@]7(C)CC[C@@H](O)C9)(C)[C@@]8([H])CC6)=O)=O)C(NCCNC(C%10=NC=CC(OC%11=CC=C(NC(NC%12=CC=C(Cl)C(C(F)(F)F)=C%12)=O)C=C%11)=C%10)=O)=O)N=N5)=O)CC4)=O)=O)C(C%13=CC=C(OC)C=C%13OC(C)C)=N2)C=C1
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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)
NTLiverTac PDE6D degrader-1 Related Classifications
HY-174379 Related Classifications
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