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  3. Narciclasine

Narciclasine  (Synonyms: Lycoricidinol)

Cat. No.: HY-16563 Purity: 99.88%
COA Handling Instructions

Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.

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

Narciclasine Chemical Structure

Narciclasine Chemical Structure

CAS No. : 29477-83-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 578 In-stock
Solution
10 mM * 1 mL in DMSO USD 578 In-stock
Solid
1 mg USD 128 In-stock
5 mg USD 525 In-stock
10 mg USD 898 In-stock
50 mg   Get quote  
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Customer Review

Based on 11 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.

IC50 & Target[1]

ROCK

 

In Vitro

Narciclasine activates Rho and stress fibers in glioblastoma multiforme cells. The mean IC50 of ~50 nM calculated on the 6 human glioblastoma multiforme (U373, Hs683, GL19, GL5, GL16, GL17), The mean IC50 value of 47 nM for Narciclasine across a panel of 60 cancer cell lines[1]. Bioassay-guided fractionation of the A. belladonna extract resulted in the identification of lycorine as the bio-active compound. The IC50 measured for radicle growth inhibition is 0.1 μM for Narciclasine[2].

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

In Vivo

The i.v. regimen of Narciclasine at 1 mg/kg significantly (P=0.02) increases the survival of GL19 glioblastoma multiforme-bearing mice. Narciclasine when given orally at the same dose five times a week for 5 consecutive weeks also significantly increases animal survival in this model (P=0.008). Oral treatment with Narciclasine at 1 mg/kg significantly increases the survival (P=0.004) of Hs683 glioblastoma multiforme-bearing mice. Increasing the number of doses administered per week does not increase the survival of these Hs683 glioblastoma multiforme-bearing mice. Narciclasine appears to show similar increased survival in these models to temozolomide but at appreciable lower doses and following both oral and i.v. administration[1].

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

Molecular Weight

307.26

Formula

C14H13NO7

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1N[C@@]2([H])[C@H](O)[C@H](O)[C@@H](O)C=C2C3=C1C(O)=C4C(OCO4)=C3

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 26 mg/mL (84.62 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2546 mL 16.2729 mL 32.5457 mL
5 mM 0.6509 mL 3.2546 mL 6.5091 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 1.67 mg/mL (5.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.67 mg/mL (5.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.88%

References
Kinase Assay
[1]

The RhoA G-LISA assay is used. The assay uses a 96-well plate coated with the Rho binding domain of Rho family effector proteins. The active GTP-bound form of the Rho family protein but not the inactive GDP-bound form from biological samples will bind to the plate. Bound active Rho family protein is then detected by incubation with a specific primary antibody followed by a secondary antibody conjugated to horseradish peroxidase. The signal is then developed using OPD. U373 and GL19 glioblastoma multiforme cells are serum starved for 24 h and left untreated or treated with Narciclasine (100 nM) for 3 min, 5 min, 30 min, 1 h, and 2 h or treated with 2.0 μg/mL of the cell-permeable Rho inhibitor for 4 h in serum-free medium at 37°C with and without subsequent Narciclasine treatment. This product consists of highly purified C3 transferase covalently linked to a proprietary cell-penetrating moiety via a disulfide bond. The cell-penetrating moiety allows rapid and efficient transport through the plasma membrane. Once in the cytosol, the cell-penetrating moiety is released, thereby allowing C3 transferase to freely diffuse intracellularly and inactive RhoA, RhoB, and RhoC but not related GTPases such as Cdc42 or Rac1. C3 transferase inhibits Rho proteins by ADP ribosylation on Asn41 in the effector binding domain of the GTPase. Cells are then lysed and RhoA activity is measured by the RhoA G-LISA Activation Assay or alternatively cells are stained for F-actin[1].

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

Cell Assay

Cell[1]The Narciclasine IC50 concentration, the Narciclasine concentration that decreased by 50% the global growth rate of a given cell population, is assessed with the MTT assay. The cells are incubated for 72 h in the presence and absence of the Narciclasine (with concentrations ranging between 10-9 and 10-5 M concentrate) for the determination of Narciclasine IC50 values[1].

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

Animal Administration
[1]

Mice[1]
The Hs683 cell line and GL19 primoculture grafted into the brains of nude immunodeficient mice both produced invasive brain tumors. Xenograft-bearing mice receive vehicle alone, oral temozolomide at 40 mg/kg (5 administrations per week for 5 consecutive weeks), or Narciclasine at 1 mg/kg either oral (once per week for 5 weeks) or i.v. (twice per week for 5 weeks). Drug administration is initiated respectively on days 5 and 7 post-tumor grafting for the Hs683 and GL19 models. The temozolomide dose and treatment schedule are selected based on previous optimized regimens. Narciclasine dose and treatment schedule are selected based on Narciclasine toxicity study in rats after oral administration and pharmacokinetic study that we have recently published. In toxicity study, Narciclasine (25, 10, or 1 mg/kg) is administered five times a week for 3 weeks and the no adverse effect level dose is defined to be 1 mg/kg/d p.o., with minimal acanthosis reactive changes and minor variations in some biochemistry parameters observed at this dose level considered to be nonadverse.

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

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2546 mL 16.2729 mL 32.5457 mL 81.3643 mL
5 mM 0.6509 mL 3.2546 mL 6.5091 mL 16.2729 mL
10 mM 0.3255 mL 1.6273 mL 3.2546 mL 8.1364 mL
15 mM 0.2170 mL 1.0849 mL 2.1697 mL 5.4243 mL
20 mM 0.1627 mL 0.8136 mL 1.6273 mL 4.0682 mL
25 mM 0.1302 mL 0.6509 mL 1.3018 mL 3.2546 mL
30 mM 0.1085 mL 0.5424 mL 1.0849 mL 2.7121 mL
40 mM 0.0814 mL 0.4068 mL 0.8136 mL 2.0341 mL
50 mM 0.0651 mL 0.3255 mL 0.6509 mL 1.6273 mL
60 mM 0.0542 mL 0.2712 mL 0.5424 mL 1.3561 mL
80 mM 0.0407 mL 0.2034 mL 0.4068 mL 1.0171 mL
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Narciclasine Related Classifications

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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