1. Neuronal Signaling Metabolic Enzyme/Protease
  2. Cholinesterase (ChE) Beta-secretase Phosphodiesterase (PDE)
  3. Sophoflavescenol

Sophoflavescenol 

Cat. No.: HY-N2284 Purity: 98.15%
COA Handling Instructions

Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.

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

Sophoflavescenol Chemical Structure

Sophoflavescenol Chemical Structure

CAS No. : 216450-65-6

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1 mg USD 264 In-stock
5 mg USD 792 In-stock
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.

IC50 & Target

BACE1

 

AChE

 

BChE

 

PDE5

 

In Vitro

Sophoflavescenol shows cytotoxicity against human leukaemia (HL-60), Lewis lung carcinoma (LLC), and human lung adenocarcinoma epithelial (A549) cells. Sophoflavescenol exerts notable anti-inflammatory activity by inhibiting nitric oxide generation and tert-butylhydroperoxide-induced ROS generation rather than inhibiting nuclear factor kappa B activation in RAW 264.7 cells[1]. Sophoflavescenol exhibits remarkable inhibition of RLAR activity with an IC50 value of 0.30 µM, compared with 0.07 µM for epalrestat, a well known ARI. Sophoflavescenol also shows potent inhibitory activity with an IC50 value of 0.17 µM, comparable to epalrestat (0.15 µM) in the HRAR assay. In the AGE assay, sophoflavescenol (IC50 17.89 µg/mL) is a more potent inhibitor of AGE formation than aminoguanidine (IC50 81.05 µg/mL). Sophoflavescenol exerts both potent AChE and BChE inhibitory effects with respective IC50 values of 8.37 and 8.21 µM. Sophoflavescenol also exhibits good BACE1 inhibition in a dose-dependent manner with an IC50 value of 10.98 µM[2]. Sophoflavescenol is a mixed inhibitor (Ki=0.005 μM) against cGMP PDE5. Sophoflavescenol shows greatest selectivity toward PDE5, 31.5- and 196.2-fold over PDE3 and PDE4, respectively[3].

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

In Vivo

Sophoflavescenol exerts potent in vivo antitumor activity by tumor growth inhibition in the LLC tumor model as well as apoptotic activity by caspase-3 activation in HL-60 cells[1].

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

Molecular Weight

368.38

Formula

C21H20O6

CAS No.
Appearance

Solid

SMILES

O=C1C(O)=C(C2=CC=C(O)C=C2)OC3=C(C/C=C(C)\C)C(O)=CC(OC)=C13

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (67.86 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7146 mL 13.5729 mL 27.1459 mL
5 mM 0.5429 mL 2.7146 mL 5.4292 mL
10 mM 0.2715 mL 1.3573 mL 2.7146 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: 2.5 mg/mL (6.79 mM); Clear solution; Need ultrasonic

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 98.15%

References
Kinase Assay
[2]

Briefly, a mixture of 10 µL of assay buffer (50 mm sodium acetate, pH 4.5), 10 µL of BACE1 (1.0 U/mL), 10 µL of the substrate (750 nm Rh-EVNLDAEFK-Quencher in 50 mm, ammonium bicarbonate) and 10 µL of the tested samples [final concentration (f.c.) 100 µM for compounds] dissolved in 10% DMSO is incubated for 60 min at 25°C in the dark. The proteolysis of two fluorophores (Rh-EVNLDAEFK-Quencher) by BACE1 is monitored by formation of the fluorescent donor (Rh-EVNL) that increased in fluorescence wavelengths at 530-545 nm (excitation) and 570-590 nm (emission), respectively. Fluorescence is measured with a microplate spectrofluorometer. The mixture is irradiated at 545 nm and the emission intensity recorded at 585 nm. The percent inhibition (%) is obtained by the following equation: % Inhibition=[1 − (S60 − S0)/(C60 − C0)] × 100, where C60 is the fluorescence of the control (enzyme, buffer, substrate) after 60 min of incubation, C0 the initial fluorescence of the control, S60 the fluorescence of the tested samples (enzyme, sample solution, substrate) after 60 min of incubation, and S0 the initial fluorescence of the tested samples. To allow for the quenching effect of the samples, the sample solution is added to reaction mixture C, and any reduction in fluorescence by the sample is then investigated. The BACE1 inhibitory activity of each sample is expressed in terms of the IC50 value (µM required to inhibit proteolysis of the BACE1 substrate, by 50%), as calculated from the log-dose inhibition curve.

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

References
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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.

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Product Name:
Sophoflavescenol
Cat. No.:
HY-N2284
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