1. PI3K/Akt/mTOR NF-κB Apoptosis
  2. PI3K Akt NF-κB Bcl-2 Family Apoptosis
  3. Nogo-B-IN-1

Nogo-B-IN-1 ((S,R)-4v) is a covalent Nogo-B inhibitor. Nogo-B-IN-1 inhibits the progression of osteosarcoma (OS) by suppressing Nogo-B activity and the PI3K/AKT/NF-κB/Bcl-2 signaling pathway. Nogo-B-IN-1 inhibits the proliferation of OS 143B cells (IC50 = 0.28 µM) and induces apoptosis. Nogo-B-IN-1 can be used for OS targeting research.

For research use only. We do not sell to patients.

Nogo-B-IN-1

Nogo-B-IN-1 Chemical Structure

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Description

Nogo-B-IN-1 ((S,R)-4v) is a covalent Nogo-B inhibitor. Nogo-B-IN-1 inhibits the progression of osteosarcoma (OS) by suppressing Nogo-B activity and the PI3K/AKT/NF-κB/Bcl-2 signaling pathway. Nogo-B-IN-1 inhibits the proliferation of OS 143B cells (IC50 = 0.28 µM) and induces apoptosis. Nogo-B-IN-1 can be used for OS targeting research[1].

In Vitro

Nogo-B-IN-1 (0-3 μM, 24 h) inhibits the migration and proliferation, induces abnormal cell morphology, cellular shrinkage, disordered arrangement, apoptosis depends on Nogo-B in 143B cells[1].
Nogo-B-IN-1 (50 μM) inhibits Nogo-B expression, with inhibitory activity of 99% in 143B cells[1].
Nogo-B-IN-1 (0-3 μM, 24 h) can blunt Nogo-B, which in turn impairs PI3K/AKT and NF-κB activities in 143B cells[1].

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

Cell Migration Assay [1]

Cell Line: 143B cells
Concentration: 0 nM, 300 nM, 1000 nM
Incubation Time: 24 h
Result: Decreased the percentage of intercellular wound healing distance, decreased the colony growth.

Apoptosis Analysis[1]

Cell Line: 143B cells
Concentration: 0 nM, 300 nM, 1000 nM
Incubation Time: 24 h
Result: Induced apoptosis.

Western Blot Analysis[1]

Cell Line: 143B cells
Concentration: 0, 0.3, 0.5, 1, 3 μM
Incubation Time: 0, 24, 48, 72 h
Result: Downregulated Nogo-B protein level, enhanced the stability of Nogo-B.
Decreased p65, Bcl-2 protein, inhibited activation of PI3K, AKT, and p-AKT.

RT-PCR[1]

Cell Line: 143B cells
Concentration: 0, 0.3, 0.5, 1, 3 μM
Incubation Time: 24 h
Result: Had no effect of Nogo-B mRNA level.
In Vivo

Nogo-B-IN-1 (30 mg/kg, i.p., once a day, 23 days) suppresses OS progression without obvious toxicity in 143B xenograft BALB/c nude mice model[1].
Nogo-B-IN-1 (30 mg/kg, i.p., once a day, 23 days) is weakened the inhibitory effect of tumor volume and tumor weight in 43B with Nogo-B knockdown xenograft BALB/c nude mice model[1].

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

Animal Model: 143B (5 ×106) xenograft BALB/c nude mice (3-month-old) model[1]
Dosage: 30 mg/kg
Administration: i.p., once a day, 23 days
Result: Suppressed tumor growth, had no discernible morphological changes in the heart, liver, spleen, or kidney tissues.
Animal Model: 143B (5 ×106) with Nogo-B knockdown xenograft BALB/c nude mice (3-month-old) model[1]
Dosage: 30 mg/kg
Administration: i.p., once a day, 23 days
Result: Was weakened the inhibitory effect of tumor volume and tumor weight.
Molecular Weight

605.89

Formula

C29H27Cl3N2O6

SMILES

O=C(OC)[C@@](C1=CC=C(Cl)C=C1Cl)(OCC2=CC=CC=C2Cl)[C@@H](NC3=CC=C(NC(C=C)=O)C=C3)C(OCC)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    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.

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Nogo-B-IN-1
Cat. No.:
HY-175317
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