Icerguastat (Synonyms: Sephin1; IFB-088)

Name: Icerguastat
Brand: MedChemExpress
SKU: HY-111022
Rating: 5.0 (3 reviews)

Cat. No.: HY-111022 Purity: 99.93%: Data Sheet
COA

SDS
Handling Instructions
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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.

CAS No. : 951441-04-6

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Icerguastat:

(E/Z)-Icerguastat In-stock
(E/Z)-Icerguastat hydrochloride Get quote
Icerguastat Carbonate Get quote

3 Publications Citing Use of MCE Icerguastat

Cell Imaging/Staining

In Vivo Efficacy Study

Histological Imaging/Staining

: Icerguastat purchased from MedChemExpress. Usage Cited in: JACC Basic Transl Sci. 2025 Dec 15;11(1):101433. [Abstract]; Icerguastat (Sephin1) (0.5 μM; 14 d) significantly reduced calcium deposition by 47% and decreased calcium concentration by 40% in AVIC treated with OGM.

: Icerguastat purchased from MedChemExpress. Usage Cited in: JACC Basic Transl Sci. 2025 Dec 15;11(1):101433. [Abstract]; Icerguastat (Sephin1) (0.5 μM; 14 d) markedly reduced the protein levels of calcification markers OPN and Runx2 in AVICs treated with OGM.

: Icerguastat purchased from MedChemExpress. Usage Cited in: JACC Basic Transl Sci. 2025 Dec 15;11(1):101433. [Abstract]; Icerguastat (Sephin1) (1 mg/kg; i.p.; once daily for 10 d) significantly alleviated aortic stenosis in CAVD mice subjected to the adenine/Vitamin D regimen, as evidenced by marked reductions in transvalvular peak jet velocity and transaortic valve pressure.

: Icerguastat purchased from MedChemExpress. Usage Cited in: JACC Basic Transl Sci. 2025 Dec 15;11(1):101433. [Abstract]; Icerguastat (Sephin1) (1 mg/kg; i.p.; once daily for 10 d) led to the observed mitigation of calcified nodule formation in the AVs of CAVD mice.

: Icerguastat purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jun 30.; Icerguastat (Sephin1) (10 mg/kg; i.p.; once daily for 28 d) significantly improved the sensorimotor coordination and fatigue resistance of ICH (intracerebral hemorrhage) mice.

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Description

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.

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.

Molecular Weight

196.64

Formula

C₈H₉ClN₄

CAS No.

951441-04-6

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
10 mM	0.5085 mL	2.5427 mL	5.0854 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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

Purity: 99.93%

Select Batch:

Data Sheet (274 KB) SDS (420 KB)

COA (246 KB) HNMR (247 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Chen Y, et al. Sephin1, which prolongs the integrated stress response, is a promising therapeutic for multiple sclerosis. Brain. 2019;142(2):344-361. [Content Brief]

[2]. Das I, et al. Preventing proteostasis diseases by selective inhibition of a phosphatase regulatory subunit. Science. 2015;348(6231):239-242. [Content Brief]

[3]. Thapa S, et al. Sephin1 Reduces Prion Infection in Prion-Infected Cells and Animal Model. Mol Neurobiol. 2020;57(5):2206-2219. [Content Brief]

Complete Stock Solution Preparation Table

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

Icerguastat Related Classifications

Inflammation/Immunology Infection

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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Icerguastat (Synonyms: Sephin1; IFB-088)

Customer Review

Other Forms of Icerguastat:

Icerguastat Related Antibodies

3 Publications Citing Use of MCE Icerguastat

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Icerguastat Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Icerguastat Related Classifications

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