ISRIB (trans-isomer), Inhibitor of “Integrated Stress Response” (ISR)


Catalog No. size PriceQuantity
M60125-2D 10 mM in DMSO (0.443 mL) $129
M60125-2S 2 mg solid $129
M60125-10S 10 mg solid $510

Description

ISRIB (trans-isomer), the trans-isomer of ISRIB, is a potent and selective PERK inhibitor with IC50 of 5 nM and does not have global effects on translation, transcription, or mRNA stability in non-stressed cells.

Product information

CAS Number: 1597403-47-8

Molecular Weight: 451.34

Formula: C22H24Cl2N2O4

Chemical Name: N,N'-((1r,4r)-cyclohexane-1,4-diyl)bis(2-(4-chlorophenoxy)acetamide)

Smiles: O=C(COC1C=CC(Cl)=CC=1)N[C@@H]1CC[C@H](CC1)NC(=O)COC1C=CC(Cl)=CC=1

InChiKey: HJGMCDHQPXTGAV-IYARVYRRSA-N

InChi: 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)/t17-,18-

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

ISRIB blocks production of endogenous ATF4, whereas XBP1 mRNA splicing and XBP1s production persisted. ISRIB prevents cells from re-establishing ER homeostasis by blocking signaling through the PERK branch of the UPR, and decreases the viability of cells that are subjected to ER-stress.

In Vivo:

ISRIB shows favorable properties in pharmacokinetic profiling experiments and good bioavailability in vivo. ISRIB (0.25 mg/kg i.p.) increases long-term memory in mice by enhancing spatial and fear-associated learning.

References:

  1. Sidrauski C, et al. Pharmacological brake-release of mRNA translation enhances cognitive memory. (2013) Elife. 2:e00498.

Products are for research use only. Not for human use.

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