1. Cell Cycle/DNA Damage
  2. Separase
  3. Sepin-1

Sepin-1 is a potent separase inhibitor with an IC50 value of 14.8 µM. Sepin-1 inhibits cell proliferation, migration and wound healing. Sepin-1 decreases the expression of FoxM1 protein and mRNA level. Sepin-1 shows anti-tumor activity.

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

Sepin-1 Chemical Structure

Sepin-1 Chemical Structure

CAS No. : 163126-81-6

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5 mg USD 100 In-stock
10 mg USD 160 In-stock
25 mg USD 350 In-stock
50 mg USD 580 In-stock
100 mg USD 1020 In-stock
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

Sepin-1 is a potent separase inhibitor with an IC50 value of 14.8 µM. Sepin-1 inhibits cell proliferation, migration and wound healing. Sepin-1 decreases the expression of FoxM1 protein and mRNA level. Sepin-1 shows anti-tumor activity[1][2].

IC50 & Target

IC50: 14.8 µM (separase)[2]

In Vitro

Sepin-1 (0, 20, 40 µM; 24 h) inhibits cell migration and wound healing, and causes DNA damage[1].
Sepin-1 (0, 10, 20, 40 µM; 24 h) decreases the expression of FoxM1 protein and mRNA level in a dose-dependent manner[1].
Sepin-1 (0, 10, 20, 40 µM; 24 h) inhibits the expression of Plk1, Cdk1, pericentrin, Aurora, and Lamin B1 protein levels[1].

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

Cell Proliferation Assay[1]

Cell Line: BT-474, MCF7, MDA-MB-231, MDA-MB-468 cells
Concentration: 0-64 µM
Incubation Time: 3 days
Result: Inhibited cell growth with EC50s of 18.03, 17.66, 27.33, 27.92 µM for BT-474, MCF7, MDA-MB-231, MDA-MB-468 cells, respectively.

Western Blot Analysis[1]

Cell Line: BT-474, MCF7, MDA-MB-231, MDA-MB-468 cells
Concentration: 0, 10, 20, 40 µM
Incubation Time: 24 h
Result: Decreased the expression of FoxM1 protein in a dose-dependent manner, and decreased teh expression of A-Raf, B-Raf, and C-Raf.
In Vivo

Sepin-1 (10 mg/kg; i.v.; daily for 5 days a week for 3 weeks) shows anti-tumor activity in mice[2].

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

Animal Model: SCID beige mice (MCF7 xenografts)[2]
Dosage: 10 mg/kg
Administration: I.v.; daily for 5 days a week for 3 weeks
Result: Inhibited tumor growth.
Molecular Weight

223.19

Formula

C9H9N3O4

CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

[O-][N+]1=C2C(C=C(C=C2)[N+]([O-])=O)=[N+](C1(C)C)[O-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (448.05 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 4.4805 mL 22.4024 mL 44.8049 mL
5 mM 0.8961 mL 4.4805 mL 8.9610 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. 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)

Mass
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Concentration
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Volume
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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

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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (11.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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
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. 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 4.4805 mL 22.4024 mL 44.8049 mL 112.0122 mL
5 mM 0.8961 mL 4.4805 mL 8.9610 mL 22.4024 mL
10 mM 0.4480 mL 2.2402 mL 4.4805 mL 11.2012 mL
15 mM 0.2987 mL 1.4935 mL 2.9870 mL 7.4675 mL
20 mM 0.2240 mL 1.1201 mL 2.2402 mL 5.6006 mL
25 mM 0.1792 mL 0.8961 mL 1.7922 mL 4.4805 mL
30 mM 0.1493 mL 0.7467 mL 1.4935 mL 3.7337 mL
40 mM 0.1120 mL 0.5601 mL 1.1201 mL 2.8003 mL
50 mM 0.0896 mL 0.4480 mL 0.8961 mL 2.2402 mL
60 mM 0.0747 mL 0.3734 mL 0.7467 mL 1.8669 mL
80 mM 0.0560 mL 0.2800 mL 0.5601 mL 1.4002 mL
100 mM 0.0448 mL 0.2240 mL 0.4480 mL 1.1201 mL
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Sepin-1 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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Sepin-1
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HY-117522
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