1. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
    Metabolic Enzyme/Protease
  2. Sirtuin
    Apoptosis
    Phospholipase
  3. Cambinol

Cambinol 

Cat. No.: HY-100732 Purity: 99.70%
Handling Instructions

Cambinol est un inhibiteur SIRT1 et SIRT2 avec des valeurs IC50 de 56 μM et 59 μM, respectivement.

Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 μM and 59 μM, respectively. Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).

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

Cambinol Chemical Structure

Cambinol Chemical Structure

CAS No. : 14513-15-6

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10 mM * 1 mL in DMSO USD 71 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
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10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
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100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 μM and 59 μM, respectively. Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[1][2].

IC50 & Target[1]

SIRT1

56 μM (IC50)

SIRT2

59 μM (IC50)

In Vitro

Cambinol inhibits NAD-dependent deacetylase activity of human SIRT1 and SIRT2. Inhibition of SIRT1 activity with cambinol during genotoxic stress leads to hyperacetylation of key stress response proteins and promotes cell cycle arrest. Treatment of BCL6-expressing Burkitt lymphoma cells with cambinol as a single agent induces apoptosis, which is accompanied by hyperacetylation of BCL6 and p53. Cambinol has only weak inhibitory activity against SIRT5 (42% inhibition at 300 μM) and no activity against SIRT3[1].

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

In Vivo

Cambinol is well tolerated in mice (100 mg/kg) and inhibits growth of Burkitt lymphoma xenografts. No significant weight loss occurs in cambinol-treated animals relative to controls. Inhibitors of NAD-dependent deacetylases may constitute novel anticancer agents[1].

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

Molecular Weight

360.43

Formula

C₂₁H₁₆N₂O₂S

CAS No.

14513-15-6

SMILES

O=C(C(CC1=C2C=CC=CC2=CC=C1O)=C(C3=CC=CC=C3)N4)NC4=S

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (138.72 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7745 mL 13.8723 mL 27.7446 mL
5 mM 0.5549 mL 2.7745 mL 5.5489 mL
10 mM 0.2774 mL 1.3872 mL 2.7745 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.77 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.77 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

.The reporter construct with or without varying amounts of GAL4-BCL6 expression plasmid are introduced into NCI-H460 cells using calcium phosphate method. A plasmid containing cytomegalovirus (CMV)-driven β-galactosidase reporter (50 ng) is cotransfected to control for transfection efficiency. Sixteen hours after transfection, cells are treated with 100 μM cambinol of DMSO (control) for 24 hours and the luciferase and β-galactosidase activity is measured[1].

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

Animal Administration
[1]

Mice: Cambinolat the dose of 100 mg/kg, or vehicle are administered i.v. through tail vein injection or i.p. daily from day 5 to 19 (five injections per week). The dose of 100 mg/kg cambinol is the highest dose that could be administered as a single i.v. injection due to limited solubility of the drug. Tumor size is measured thrice a week using caliper and the tumor volumes are calculated[1].

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

References

Purity: 99.70%

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Keywords:

CambinolSirtuinApoptosisPhospholipaseInhibitorinhibitorinhibit

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