2. PROTAC Metabolic Enzyme/Protease Apoptosis Stem Cell/Wnt Neuronal Signaling Cell Cycle/DNA Damage Epigenetics
  3. Molecular Glues E1/E2/E3 Enzyme Apoptosis Notch PARP Caspase Bcl-2 Family Ligands for E3 Ligase
  4. 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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NEURL1B-IN-1

NEURL1B-IN-1 Chemical Structure

CAS No. : 3068938-30-4

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NEURL1B-IN-1 Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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von Hippel-Lindau (VHL) MDM2 Cereblon IAP KLHDC2 Fbxo3 RNF4 DCAF11 DCAF1 UHRF1 TRIM21 NEURL1B KLHL41

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Description

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[1].

IC50 & Target[1]

NEURL1B

 

In Vitro

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.

NEURL1B-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: HepG2, Huh-7, SK-Hep-1 and THLE-2 cells
Concentration: /
Incubation Time: /
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
In Vivo

NEURL1B-IN-1 (30-60 mg/kg; i.p., once daily for 60 consecutive days) inhibits hepatocellular carcinoma tumor growth in SK-Hep-1 xenograft nude mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice treated SK-Hep-1 cells (4-week-old)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: i.p.; daily; 60 days
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.
Molecular Weight

478.62

Formula

C30H38O5
CAS No.
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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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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NEURL1B-IN-1 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NEURL1B-IN-13068938-30-4Molecular GluesE1/E2/E3 EnzymeApoptosisNotchPARPCaspaseBcl-2 FamilyLigands for E3 LigaseE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligasepoly ADP ribose polymerase E3 ligase-recruiting MoietyArg422liver cancer cellsNotch signalingHepG2Huh-7NHR2 domainNEURL1Bhepatocellular carcinomaxenograft nude miceDLL1Inhibitorinhibitorinhibit

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