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

Icerguastat (Synonyms: Sephin1; IFB-088)

Cat. No.: HY-111022 Purity: 99.56%
Handling Instructions

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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10 mg USD 130 In-stock
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Based on 1 publication(s) in Google Scholar

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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. Sephin1 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].

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].

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.
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)

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
*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: ≥ 2.08 mg/mL (10.58 mM); Clear solution

  • 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

*All of the co-solvents are provided by MCE.
References
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Product Name:
Icerguastat
Cat. No.:
HY-111022
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