1. Cell Cycle/DNA Damage Stem Cell/Wnt MAPK/ERK Pathway
  2. Casein Kinase ERK CDK
  3. Longdaysin

Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.

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

Longdaysin Chemical Structure

Longdaysin Chemical Structure

CAS No. : 1353867-91-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 144 In-stock
25 mg USD 288 In-stock
50 mg USD 460 In-stock
100 mg USD 690 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively[1][2].

IC50 & Target[2]

CKIα

5.6 μM (IC50)

CKIδ

8.8 μM (IC50)

CDK7

29 μM (IC50)

ERK2

52 μM (IC50)

In Vitro

Longdaysin (0-9 µM; 1 week) lengthens circadian period in adult tail fibroblasts, lung explants, and SCN explants from mPer2Luc knockin mice[2].
Longdaysin (0-25 µM; 1 week ) inhibits the colony formation, migration, invasion, and sphere formation of breast cancer Hs578T or MDA-MB-231 cells[3].
Longdaysin (0-50 µM; 24 h) inhibits Wnt/β-catenin signaling by inhibition of CK1δ and CK1ε in HEK293T cells[3].

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

Western Blot Analysis[3]

Cell Line: HEK293T cells
Concentration: 0-50 µM
Incubation Time: 24 h
Result: Reduced the levels of phosphorylated LRP6, total LRP6, phosphorylated DVL2, activated β-catenin, and total β-catenin.
In Vivo

Longdaysin (0-9 µM; 1 week) increases circadian period in zebrafish[2].
Longdaysin (5 mg/kg, i.p., every 3 days for 3 weeks) inhibits tumor growth in MDA-MB-231 xenografts mice[3].

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

Animal Model: MDA-MB-231 xenografts[3]
Dosage: 5 mg/kg
Administration: i.p., every 3 days for 3 weeks
Result: Decreased tumor cell density and proliferation (indicated by Ki-67).
Reduced the expression of active and total β-catenin, and decreased the expression of phosphorylated and total LRP6, phosphorylated DVL2, and active and total β-catenin.
Reduced mRNA expression of the Wnt target genes including Axin2, DKK1, LEF1, and Survivin.
Molecular Weight

335.33

Formula

C16H16F3N5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)C1=CC=CC(CNC2=NC=NC3=C2N=CN3C(C)C)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (372.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9821 mL 14.9107 mL 29.8214 mL
5 mM 0.5964 mL 2.9821 mL 5.9643 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

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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: ≥ 2.08 mg/mL (6.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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).

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

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
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9821 mL 14.9107 mL 29.8214 mL 74.5534 mL
5 mM 0.5964 mL 2.9821 mL 5.9643 mL 14.9107 mL
10 mM 0.2982 mL 1.4911 mL 2.9821 mL 7.4553 mL
15 mM 0.1988 mL 0.9940 mL 1.9881 mL 4.9702 mL
20 mM 0.1491 mL 0.7455 mL 1.4911 mL 3.7277 mL
25 mM 0.1193 mL 0.5964 mL 1.1929 mL 2.9821 mL
30 mM 0.0994 mL 0.4970 mL 0.9940 mL 2.4851 mL
40 mM 0.0746 mL 0.3728 mL 0.7455 mL 1.8638 mL
50 mM 0.0596 mL 0.2982 mL 0.5964 mL 1.4911 mL
60 mM 0.0497 mL 0.2485 mL 0.4970 mL 1.2426 mL
80 mM 0.0373 mL 0.1864 mL 0.3728 mL 0.9319 mL
100 mM 0.0298 mL 0.1491 mL 0.2982 mL 0.7455 mL
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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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Longdaysin
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