| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: =99.07%
ISRIB, the trans-isomer of ISRIB, is a novel, potent and selective inhibitor of PERK (PRKR-like endoplasmic reticulum kinase or protein kinase R (PKR)-like endoplasmic reticulum kinase) with IC50 of 5 nM. With an IC50 value of 5 nM, ISRIB effectively counteracted the consequences of eIF2α phosphorylation. An endogenous transcription factor called ATF4 that binds to cAMP was inhibited by ISRIB. At the expense of polyribosomes brought on by endoplasmic reticulum (ER) stress, ISRIB in mouse embryonic fibroblasts (MEFs) reversed the rise in 80S monosomes. ER-stressed cells had lower cell survival when ISRIB was present. While inhibiting the formation of stress granules (SG) brought on by eIF2α phosphorylation in stressed cells, ISRIB also restored mRNA translation in these cells.
| Targets |
PERK (IC50 = 5 nM)
|
|
|---|---|---|
| ln Vitro |
|
|
| ln Vivo |
|
|
| Enzyme Assay |
In 96-well plates, U2OS cells expressing the ATF4-dGFP-IRES-Cherry reporter are placed. For an 8-hour treatment, the cells are then exposed to 100 nM Thapsigargin and 10 M of the cherry-picked compounds. An automated microscope is used to visualize stained cells after Hoechst 33,258 staining. The INCell Developer Toolbox Software, version 1.9, is used to collect data and analyze images. Compounds that prevent the ATF4-dGFP reporter from being induced, do not prevent the buildup of mCherry downstream of the IRES, and are deemed non-toxic based on cell number measured by counting nuclei are purchased again for additional testing.
|
|
| Cell Assay |
On 96-well plates, U2OS cells are plated and given the night to recover. The level of eIF2α phosphorylation is measured after treatments with 2 µg/ml tunicamycin, 100 nM thapsigargin, 100 nM ISRIB in either the presence or absence of 100 nM ISRIB, or just ISRIB.
|
|
| Animal Protocol |
|
|
| References |
| Molecular Formula |
C22H24CL2N2O4
|
|---|---|
| Molecular Weight |
451.344
|
| Exact Mass |
450.1113
|
| Elemental Analysis |
C, 58.55; H, 5.36; Cl, 15.71; N, 6.21; O, 14.18
|
| CAS # |
1597403-47-8
|
| Related CAS # |
ISRIB;548470-11-7
|
| Appearance |
Solid powder
|
| SMILES |
C1CC(CCC1NC(=O)COC2=CC=C(C=C2)Cl)NC(=O)COC3=CC=C(C=C3)Cl
|
| InChi Key |
HJGMCDHQPXTGAV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H24Cl2N2O4/c23-15-1-9-19(10-2-15)29-13-21(27)25-17-5-7-18(8-6-17)26-22(28)14-30-20-11-3-16(24)4-12-20/h1-4,9-12,17-18H,5-8,13-14H2,(H,25,27)(H,26,28)
|
| Chemical Name |
2-(4-chlorophenoxy)-N-[4-[[2-(4-chlorophenoxy)acetyl]amino]cyclohexyl]acetamide
|
| Synonyms |
ISRIB; trans-ISRIB
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 0.83 mg/mL (1.84 mM) in 50% PEG300 +50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication (<60°C).
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2216 mL | 1.1078 mL | 2.2156 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Sidrauski C, et al. Elife. 2013, 2, e00498. |
|---|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
