2. Metabolic Enzyme/Protease
  3. Phosphatase
  4. Icerguastat

Icerguastat  (Synonyms: Sephin1; IFB-088)

Cat. No.: HY-111022 Purity: 99.90%
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Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect.

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

Icerguastat Chemical Structure

Icerguastat Chemical Structure

CAS No. : 951441-04-6

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Based on 1 publication(s) in Google Scholar

Other Forms of Icerguastat:

Icerguastat Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect[1][2][3].

In Vitro

Icerguastat (5 μM) prolongs eIF2α phosphorylation in oligodendrocytes under stress[1].
Icerguastat (Sephin1) (selective inhibitor of a holophosphatase), safely and selectively inhibits a regulatory subunit of protein phosphatase 1 in vivo. Icerguastat selectively binds and inhibits the stress-induced PPP1R15A, but not the related and constitutive PPP1R15B, to prolong the benefit of an adaptive phospho-signaling pathway, protecting cells from otherwise lethal protein misfolding stress[2].

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

Icerguastat Related Antibodies
In Vivo

Icerguastat (4-8 mg/kg; i.p.; daily for 35 days) delays the onset of EAE (experimental autoimmune encephalomyelitis)[1].
Icerguastat (100 μg; i.p.) prolongs the survival of prion-infected mice[3].

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

Animal Model: C57BL/6J female mice immunized with MOG35-55/CFA to induce chronic EAE[1]
Dosage: 4 mg/kg, 8 mg/kg
Administration: I.p.; daily for 35 days
Result: Significantly delayed clinical disease onset with both dosages, but to a greater extent with the 8 mg/kg treatment.
Animal Model: Five-week-old female FVB mice (intracerebrally with mouse-adapted RML prions)[3]
Dosage: 100 μg
Administration: I.p.; 3 times per week for 60 days, after 60 days of treatment, the treatment was reduced to two i.p. injections per week for another 20 days.
Result: Significantly prolonged survival of prion-infected mice.
Clinical Trial
Molecular Weight

196.64

Formula

C8H9ClN4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=CC=C1/C=N/NC(N)=N
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 : 50 mg/mL (254.27 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 5.0854 mL 25.4272 mL 50.8544 mL
5 mM 1.0171 mL 5.0854 mL 10.1709 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.

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  • 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: ≥ 2.08 mg/mL (10.58 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% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (10.58 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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).

*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 5.0854 mL 25.4272 mL 50.8544 mL 127.1359 mL
5 mM 1.0171 mL 5.0854 mL 10.1709 mL 25.4272 mL
10 mM 0.5085 mL 2.5427 mL 5.0854 mL 12.7136 mL
15 mM 0.3390 mL 1.6951 mL 3.3903 mL 8.4757 mL
20 mM 0.2543 mL 1.2714 mL 2.5427 mL 6.3568 mL
25 mM 0.2034 mL 1.0171 mL 2.0342 mL 5.0854 mL
30 mM 0.1695 mL 0.8476 mL 1.6951 mL 4.2379 mL
40 mM 0.1271 mL 0.6357 mL 1.2714 mL 3.1784 mL
50 mM 0.1017 mL 0.5085 mL 1.0171 mL 2.5427 mL
60 mM 0.0848 mL 0.4238 mL 0.8476 mL 2.1189 mL
80 mM 0.0636 mL 0.3178 mL 0.6357 mL 1.5892 mL
100 mM 0.0509 mL 0.2543 mL 0.5085 mL 1.2714 mL
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Icerguastat 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:

Icerguastat951441-04-6Sephin1 IFB-088Sephin 1Sephin-1IFB088IFB 088IFB-088PhosphatasephosphatasestressERproteinmisfoldingsclerosiseIF2αprionInhibitorinhibitorinhibit

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