1. Autophagy
    Apoptosis
  2. Autophagy
    Apoptosis
  3. Spautin-1

Spautin-1 

Cat. No.: HY-12990 Purity: 99.26%
Handling Instructions

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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10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
5 mg USD 55 In-stock
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10 mg USD 70 In-stock
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50 mg USD 250 In-stock
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100 mg USD 450 In-stock
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Based on 1 publication(s) in Google Scholar

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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.

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].

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

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].

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

Molecular Weight

271.26

Formula

C₁₅H₁₁F₂N₃

CAS No.

1262888-28-7

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (184.33 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

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
10 mM 0.3687 mL 1.8433 mL 3.6865 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 (9.22 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.22 mM); Clear solution

*All of the co-solvents are provided by MCE.
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
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Keywords:

Spautin-1Spautin1Spautin 1AutophagyApoptosisInhibitorinhibitorinhibit

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