NEURL1B-IN-1
NEURL1B-IN-1 is a molecular glue-like NEURL1B degrader with a Kd value of 46.2 nM. NEURL1B-IN-1 binds to Arg422 within the NHR2 domain of NEURL1B, triggers its autoubiquitination and proteasomal degradation, disrupts its interaction with DLL1, and attenuates the Notch signaling pathway. NEURL1B-IN-1 induces cell cycle arrest and apoptosis, and inhibits migration of hepatocellular carcinoma cells. NEURL1B-IN-1 is applicable to research related to hepatocellular carcinoma.
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- CAS No.: 3068938-30-4
- Formule: C30H38O5
- Masse moléculaire:478.62
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
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NEURL1B |
NEURL1B-IN-1 (compound 1) potently inhibits the viability of HepG2, Huh-7 and SK-Hep-1 hepatocellular carcinoma cells[1].
NEURL1B-IN-1 (7.5 μM) potently inhibits colony formation of SK-Hep-1 (inhibition rate: 93.6%) and Huh-7 (inhibition rate: 83.9%) hepatocellular carcinoma cells[1].
NEURL1B-IN-1 (7.5 μM) significantly reduces DNA synthesis in SK-Hep-1 (by 83.9%) and Huh-7 (by 66.3%) hepatocellular carcinoma cells[1].
NEURL1B-IN-1 (2.5-7.5 μM) induces G2/M cell cycle arrest and apoptosis, and inhibits cell migration and invasion in SK-Hep-1 and Huh-7 hepatocellular carcinoma cells[1].
NEURL1B-IN-1 (2.5-7.5 μM) downregulates the protein expression levels of CyclinB1 and phosphorylated cdc2 (Tyr17) in SK-Hep-1 and Huh-7 hepatocellular carcinoma cells[1].
NEURL1B-IN-1 (2.5-7.5 μM) upregulates the expression of cleaved-PARP-1 and Bax proteins in SK-Hep-1 and Huh-7 hepatocellular carcinoma cells[1].
NEURL1B-IN-1 (7.5 μM) regulates epithelial-mesenchymal transition (EMT) by altering the protein expression of E-cadherin, Vimentin and Slug in SK-Hep-1 and Huh-7 hepatocellular carcinoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2, Huh-7, SK-Hep-1 and THLE-2 cells
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Concentration:/
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Incubation Time:/
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Result:Potently inhibited the viability of HepG2, Huh-7, and SK-Hep-1 hepatocellular carcinoma cells with IC50 values of 5.6, 4.8, and 4.6 μM respectively, and had cytotoxicity to normal THLE-2 liver cells with a CC50 of 5.5 μM
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 mice treated SK-Hep-1 cells (4-week-old)[1]
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Dosage:30 mg/kg; 60 mg/kg
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Administration:i.p.; daily; 60 days
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Result:Reduced tumor volume by 57% and tumor weight by 37% on day 60 at 30 mg/kg.
Reduced tumor volume by 69% and tumor weight by 69% on day 60 at 60 mg/kg.
Caused no significant changes in mouse body weight or liver histopathology at either dose.
Reduced proliferation marker Ki67 expression, increased apoptosis marker cleaved caspase-3 expression, downregulated NEURL1B, Notch components NICD and HES1, and EMT markers α-SMA and Vimentin, while upregulating DLL1 in tumor tissues at 60 mg/kg.
Chemical Information
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CAS No. 3068938-30-4
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Masse moléculaire 478.62
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Formule C30H38O5
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SMILES
[H][C@@]12C[C@H]3[C@H](OC([C@@]34C[C@@H]5C[C@]4(C6=C5[C@@](O)(CC[C@H]7C(C(O[C@H]67)=O)=C)C)C)=O)C[C@]1(CCCC2=C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NEURL1B-IN-1 Related Classifications
HY-182008 Related Classifications
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