2. Cell Cycle/DNA Damage Autophagy Apoptosis
  3. PERK Autophagy Apoptosis
  4. ISRIB (trans-isomer)

ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM. ISRIB potently reverses the effects of eIF2α phosphorylation (IC50=5 nM).

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

ISRIB (trans-isomer) Chemical Structure

ISRIB (trans-isomer) Chemical Structure

CAS No. : 1597403-47-8

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 143 In-stock
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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of ISRIB (trans-isomer):

ISRIB (trans-isomer) Related Antibodies

Top Publications Citing Use of Products

    ISRIB (trans-isomer) purchased from MedChemExpress. Usage Cited in: Oncogene. 2017 Nov 30;36(48):6738-6746.  [Abstract]

    ISRIB reverses the expression of β-catenin. HCT116 cells are transfected and CT26.WT cells are infected for 48 and 72 h, respectively. The cells are treated with ISRIB (100 nM) for 24 h.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM. ISRIB potently reverses the effects of eIF2α phosphorylation (IC50=5 nM).

    IC50 & Target[1]

    PERK

    5 nM (IC50)

    In Vitro

    Trans-ISRIB is 100-fold more potent (IC50=5 nM) than cis-ISRIB (IC50= 600 nM), indicating that the compound’s interaction with its cellular target is stereospecific. ISRIB reduces the viability of cells subjected to PERK-activation by chronic endoplasmic reticulum stress[1]. ISRIB substantially reverses the translational effects elicited by phosphorylation of eIF2α and induces no major changes in translation or mRNA levels in unstressed cells. eIF2α phosphorylation-induced stress granule (SG) formation is blocked by ISRIB[2].

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

    ISRIB (trans-isomer) Related Antibodies
    In Vivo

    ISRIB increases long-term memory in rodents. ISRIB-treated mice display significant enhancement in spatial and fear-associated learning. ISRIB displays a half-life in plasma of 8 hr and readily crossed the blood-brain barrier, quickly equilibrating with the central nervous system[1].

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

    451.34

    Formula

    C22H24Cl2N2O4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N[C@H]1CC[C@H](NC(COC2=CC=C(Cl)C=C2)=O)CC1)COC3=CC=C(Cl)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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 4.55 mg/mL (10.08 mM; ultrasonic and warming and heat to 60°C; 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 2.2156 mL 11.0781 mL 22.1562 mL
    5 mM 0.4431 mL 2.2156 mL 4.4312 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    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:

    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% Saline

      Solubility: 0.83 mg/mL (1.84 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

    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.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 98.58%

    COA (243 KB) RP-HPLC (246 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    U2OS cells are plated on 96-well plates and left to recover overnight. Cells are treated with either with 2 µg/ml tunicamycin or 100 nM thapsigargin in the presence or absence of 100 nM ISRIB or with ISRIB alone for the indicated and the level of eIF2α phosphorylation is determined[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice: Intra-peritoneal (ip) route of administration is performed on 6-7 wk old female CD-1 mice. Animals receives a single, 5 mg/kg dose in groups of three mice/compound/route of administration. ISRIB is dissolved in DMSO then diluted 1:1 in Super-Refined PEG 400. Blood (80 μL) is collected from the saphenous vein at intervals post-dosing (20 min, 1 hr, 3 hr, 8 hr, 24 hr) in EDTA containing collection tubes and plasma is prepared for analysis. Compounds are detected by time-of-flight mass spectroscopy[1].

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2156 mL 11.0781 mL 22.1562 mL 55.3906 mL
    5 mM 0.4431 mL 2.2156 mL 4.4312 mL 11.0781 mL
    10 mM 0.2216 mL 1.1078 mL 2.2156 mL 5.5391 mL
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    ISRIB (trans-isomer) 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:

    ISRIB (trans-isomer)1597403-47-8PERKAutophagyApoptosisProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseInhibitorinhibitorinhibit

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