2. Metabolic Enzyme/Protease Neuronal Signaling NF-κB Immunology/Inflammation Apoptosis
  3. Lipoxygenase Amyloid-β Reactive Oxygen Species (ROS) Apoptosis
  4. CNB-001

CNB-001 is a potent and orally active 5-lipoxygenase (5-LOX) inhibitor. CNB-001 can decreases 5-LOX expression and increase proteasome activity. CNB-001 can inhibit accumulation of soluble Amyloid-β and ubiquitinated aggregated proteins. CNB-001 can inhibit apoptosis, ROS production and stabilize mitochondrial membrane potential. CNB-001 can reduce insulin resistance and increase glucose uptake. CNB-001 also exhibits anti-ischemic, anti-inflammatory effects. CNB-001 can be used for the researches of inflammation, neurological and metabolic disease, such as Alzheimer's disease, stroke and diabetes.

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CNB-001

CNB-001 Chemical Structure

CAS No. : 1019110-87-2

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CNB-001 Related Antibodies

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Description

CNB-001 is a potent and orally active 5-lipoxygenase (5-LOX) inhibitor. CNB-001 can decreases 5-LOX expression and increase proteasome activity. CNB-001 can inhibit accumulation of soluble Amyloid-β and ubiquitinated aggregated proteins. CNB-001 can inhibit apoptosis, ROS production and stabilize mitochondrial membrane potential. CNB-001 can reduce insulin resistance and increase glucose uptake. CNB-001 also exhibits anti-ischemic, anti-inflammatory effects. CNB-001 can be used for the researches of inflammation, neurological and metabolic disease, such as Alzheimer's disease, stroke and diabetes[1][2][3][4].

IC50 & Target[1][2]

5-LOX

70 nM (IC50)

15-LOX

 

In Vitro

CNB-001 (1 μM, 24-96 h) inhibits and promotes the clearance of Aβ aggregation in MC65 cells[1].
CNB-001 (1 μM, 48 h) activates three proteasome activities (chymotrypsin-like, trypsin-like, caspase-like) and degrades Aβ in MC65 cells[1].
CNB-001 (1 μM, 1-24 h) induces eIF2α (Ser51) phosphorylation and increases ATF4 expression in MC65 cells[1].
CNB-001 (1 μM, 1-24 h) inhibits 5-lipoxygenase (5-LOX, IC50 = 70 nM) and increases S523 phosphorylation and decreases S271 phosphorylation of 5-LOX in MC65 cells[1].
CNB-001 inhibits leukotriene B4 (LTB4) production in human peripheral blood mononuclear lymphocytes (PBML) with an IC50 of 0.076 μM[2].
CNB-001 (0-2 μM) inhibits 15-LOX in rabbit reticulocytes[2].
NB-001 (0.5-15 μM, 24 h) exhibits a half-toxic concentration (TC50) of 15.3 μM in quiescent C2C12 myotubes[3].
CNB-001 (1 μM, 12 h) reverses Palmitic acid (HY-N0830)-induced insulin resistance and restores insulin-stimulated glucose uptake in C2C12 myotubes[3].
CNB-001 protects SK-N-SH human neuroblastoma cells against Rotenone (HY-B1756)-induced neurotoxicity by inhibiting intracellular ROS generation, apoptosis and stabilizing mitochondrial membrane potential[4].

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

CNB-001 Related Antibodies

Western Blot Analysis[1]

Cell Line: MC65 cells
Concentration: 1 μM
Incubation Time: 1, 2, 4 and 6 h
Result: Increased S523 phosphorylation and decreases S271 phosphorylation of 5-LOX.
In Vivo

CNB-001 (25 mg/kg diet, p.o., daily for 6 months) improves the working memory in APPswe/PS1E9 transgenic mice[1].
CNB-001 (500 mg/kg, p.o., 30 mins before Aβ1-42 injection) completely reverses the contextual memory impairment in mice injected with Aβ1-42[1].
CNB-001 (5-50 mg/kg, i.v., 5 or 60 mins post-embolization) improves behavioral deficits in New Zealand white rabbits with embolic stroke[2].
CNB-001 (10 mg/kg, i.v., 5 mins after MCAO) reduces infarct expansion in cynomolgus monkeys with permanent middle cerebral artery occlusion (MCAO)[2].
CNB-001 (40 mg/kg, i.p., daily except weekends for 20-22 weeks) alleviates high-fat diet-induced obesity and insulin resistance in C57BL/6J mice[3].
CNB-001 (24 mg/kg, i.p., daily from day 1 to day 7) mitigates motor impairments and neurotoxicity in MPTP-induced Parkinson’s disease (PD) mice[4].

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

Animal Model: APPswe/PS1E9 transgenic models[1]
Dosage: 25 mg/kg diet
Administration: Orally administration, daily for 6 months
Result: Increased arm alternation choices.
Increased eIF2α phosphorylation, ATF4 and HSP90 expression in the hippocampus.
Reduced soluble Aβ1-42 (50%) and ubiquitinated aggregated proteins.
Increased the expression of synapse-associated proteins (phosphorylated synapsin-1, Pro-BDNF, Homer1).
Decreased the expression of clusterin and 5-LOX (>40%).
Animal Model: New Zealand white rabbits with embolic stroke[2]
Dosage: 5-50 mg/kg 1 h post-embolization and 10 mg/kg 5 min post-embolization
Administration: Intravenously injection
Result: Increased P50 (clot burden causing 50% neurological dysfunction) by 74%.
Decreased COX-2 and 5-LOX expression, and increased BDNF levels in ipsilateral cortical tissues.
Animal Model: High-fat diet-induced obesity and insulin resistance in C57BL/6J mice models[3]
Dosage: 40 mg/kg
Administration: Intraperitoneally injection, daily except weekends for 20-22 weeks
Result: Reduced body weight gain (without altering food intake).
Decreased serum triglyceride and interleukin-6 (IL-6) levels.
Improved glucose tolerance (lowers IPGTT AUC) and insulin sensitivity (lowers IPITT AUC).
Restored insulin-stimulated glucose uptake in gastrocnemius muscle.
Upregulated insulin signaling molecules (p-IR, p-Akt) and downregulates protein-tyrosine phosphatase 1B (PTP1B) and phospho-eIF2α in skeletal muscle.
Attenuated hepatic steatosis (reduces liver triglycerides and Oil Red O-stained fat droplets), and increased energy expenditure (without changing respiratory exchange ratio, RER).
Animal Model: MPTP-induced Parkinson’s disease (PD) mice[4]
Dosage: 24 mg/kg
Administration: Intraperitoneally injection, daily from day 1 to day 7
Result: Reduced runway crossing time and foot slip errors in the narrow beam test.
Shortened fixed posture duration and reduced latency to shift four limbs.
Restored striatal dopamineand its metabolites (DOPAC, HVA) levels.
Decreased nitrite and citrulline accumulation.
Downregulated pro-inflammatory factors (TNF-α, IL-1β, IL-6, iNOS, GFAP, COX-2) and pro-apoptotic markers (Bax, cytochrome C, cleaved caspase-3).
Upregulated anti-apoptotic Bcl-2, and increased dopamine transporter (DAT) immunoreactivity in the substantia nigra (SN) and striatum (ST).
Molecular Weight

440.49

Formula

C27H24N2O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C(C=C1OC)/C=C/C2=NN(C3=CC=CC=C3)C(/C=C/C4=CC(OC)=C(O)C=C4)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation
References
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CNB-001 Related Classifications

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Help & FAQs
  • 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.

Keywords:

CNB-0011019110-87-2CNB001CNB 001LipoxygenaseAmyloid-βReactive Oxygen Species (ROS)ApoptosisLOXβ-amyloid peptideAβAbeta5-LOXROSMitochondrial membrane potentialInsulin resistanceAlzheimer's diseaseParkinson diseaseDiabetesNeuroinflammationInhibitorinhibitorinhibit

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