2. Autophagy Apoptosis Cell Cycle/DNA Damage
  3. Autophagy Apoptosis Deubiquitinase
  4. Spautin-1

Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC50s of 0.6-0.7 μM.

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

Spautin-1 Chemical Structure

Spautin-1 Chemical Structure

CAS No. : 1262888-28-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 67 In-stock
Solution
10 mM * 1 mL in DMSO USD 67 In-stock
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10 mg USD 77 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Spautin-1 Related Antibodies

Top Publications Citing Use of Products

View All Deubiquitinase Isoform Specific Products:

View All Isoforms
USP1 USP2 USP7 USP8 USP30 UCHL1

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC50s of 0.6-0.7 μM.

Cellular Effect
Cell Line Type Value Description References
MIA PaCa-2 EC50
20 μM
Compound: Spautin-1
Antiproliferative activity against human MIA PaCa-2 cells assessed as cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human MIA PaCa-2 cells assessed as cell viability measured after 72 hrs by MTT assay
[PMID: 28105281]
PC-9 IC50
> 5 μM
Compound: 5
Cytotoxicity against human PC-9 cells harboring EGFR mutant assessed as inhibition of cell growth incubated for 72 hrs by ATP-based luminescence CellTiter-Glo assay
Cytotoxicity against human PC-9 cells harboring EGFR mutant assessed as inhibition of cell growth incubated for 72 hrs by ATP-based luminescence CellTiter-Glo assay
[PMID: 36410591]
In Vitro

Spautin-1 enhances imatinib mesylate (IM)-induced CmL cell apoptosis by reducing the expression of the anti-apoptotic proteins Mcl-1 and Bcl-2. The pro-apoptotic activity of spautin-1 is associated with activation of GSK3β, an important downstream effector of PI3K/AKT. Spautin-1 enhances IM-induced cytotoxicity in CmL cell line K562, decreasing the IC50 from 1 to 0.5 μM[1]. The mechanism of spautin-1 acting on acute pancreatitis is associated with impaired autophagy inhibition[2].

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

Spautin-1 Related Antibodies
In Vivo

Spautin-1 ameliorates the pathogenesis of acute pancreatitis induced by cerulein or L-arginine. Spautin-1 pretreatment significantly diminishes the elevation of serum amylase and lipase levels, which are indicative of trypsin activity. Increasing levels of serum TNFα caused by cerulein are inhibited in the presence of spautin-1. Spautin-1 treatment can ameliorate the inflammation damage induced by cerulein, such as edema, degeneration, coagulative necrosis and infiltration of inflammatory cells[2].

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

271.26

Formula

C15H11F2N3
CAS No.
Appearance

Solid

Color

Light yellow to khaki

SMILES

FC1=CC2=C(N=CN=C2C=C1)NCC3=CC=C(F)C=C3
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 : 50 mg/mL (184.33 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 3.6865 mL 18.4325 mL 36.8650 mL
5 mM 0.7373 mL 3.6865 mL 7.3730 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: ≥ 2.5 mg/mL (9.22 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 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: ≥ 2.5 mg/mL (9.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% PBS

    Solubility: 10 mg/mL (36.87 mM); Suspended solution; Need ultrasonic

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
Cell Assay
[1]

Spautin-1 is dissolved in DMSO. Cell proliferation is evaluated using CCK-8 kit. K562 cells (1x105/mL) are seeded into 96-well plates in triplicate and then treated with 125 to 4,000 nM IM alone or in combi¬nation with spautin-1 (10 μM). After 48 h of incubation, 10 μL of CCK-8 reagent is added to each well. Four hours later, the absorbance is read at 450 nm using a microplate reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice: In this study, mice models with acute pancreatitis, including cerulein- and L-arginine-induced models, are constructed. For the cerulein-induced model, four intraperitoneal injections of cerulein (50 μg/kg body weight) are given consecutively at hourly intervals; The L-arginine-induced model received hourly intraperitoneal injections of 1.4 g/kg (optimal dosage for this study) L-arginine three times[2].

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 3.6865 mL 18.4325 mL 36.8650 mL 92.1625 mL
5 mM 0.7373 mL 3.6865 mL 7.3730 mL 18.4325 mL
10 mM 0.3686 mL 1.8432 mL 3.6865 mL 9.2162 mL
15 mM 0.2458 mL 1.2288 mL 2.4577 mL 6.1442 mL
20 mM 0.1843 mL 0.9216 mL 1.8432 mL 4.6081 mL
25 mM 0.1475 mL 0.7373 mL 1.4746 mL 3.6865 mL
30 mM 0.1229 mL 0.6144 mL 1.2288 mL 3.0721 mL
40 mM 0.0922 mL 0.4608 mL 0.9216 mL 2.3041 mL
50 mM 0.0737 mL 0.3686 mL 0.7373 mL 1.8432 mL
60 mM 0.0614 mL 0.3072 mL 0.6144 mL 1.5360 mL
80 mM 0.0461 mL 0.2304 mL 0.4608 mL 1.1520 mL
100 mM 0.0369 mL 0.1843 mL 0.3686 mL 0.9216 mL
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Spautin-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.

Keywords:

Spautin-11262888-28-7Spautin1Spautin 1AutophagyApoptosisDeubiquitinaseDUBsInhibitorinhibitorinhibit

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