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516535

GSK2606414

≥99% (HPLC), powder, PERK inhibitor, Calbiochem®

Synonym(s):

PERK Inhibitor I, GSK2606414

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About This Item

Empirical Formula (Hill Notation):
C24H20F3N5O
CAS Number:
1337531-89-1
Molecular Weight:
451.44
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD25976926
Assay:
≥99% (HPLC)
Form:
powder
Quality level:
200
Storage condition:
OK to freeze, protect from light
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Product Name

PERK Inhibitor I, GSK2606414, GSK2606414 is a cell-permeable, highly potent inhibitor of EIF2AK3/PERK (IC50 = 0.4 nM; [ATP] = 5 µM). Targets PERK in its inactive DFG conformation at the ATP-binding region.

Quality Level

200

assay

≥99% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

−20°C

SMILES string

O=C(CC1=CC=CC(C(F)(F)F)=C1)N2CCC3=C2C=CC(C4=CN(C)C5=C4C(N)=NC=N5)=C3

InChI

1S/C24H19F4N5O/c1-32-11-18(21-22(29)30-12-31-23(21)32)14-2-3-19-15(9-14)4-5-33(19)20(34)8-13-6-16(24(26,27)28)10-17(25)7-13/h2-3,6-7,9-12H,4-5,8H2,1H3,(H2,29,30,31)

InChI key

PXVQGBJMIQCDEX-UHFFFAOYSA-N

General description

A cell-permeable pyrrolopyrimidamine compound that acts as a highly potent EIF2AK3/PERK inhibitor (IC50 = 0.4 nM; [ATP] = 5 µM) by targeting PERK in its inactive DFG conformation at the ATP-binding region, while displaying ≥385-fold selectivity over c-Kit, Aurora B, BRK, HRI/EIF2AK1, MLK2/MAP3K10, c-MER, DDR2, PKR/EIF2AK2, and MLCK2/MYLK2 (IC50 = 154, 407, 412, 420, 452, 474, 524, 696, and 701 nM, respectively) and little activity against more than 280 other kinases (IC50 >1 µM). Shown to block ER stress-induced PERK autophosphorylation following Thapsigargin addition in A549 cultures in vitro (by 100% at ≤30 nM; 60 min preincubation) and effectively retard PxBC-3 tumor growth in mice in vivo (50 and 150 mg/kg/12 h p.o.). Also available as a 25 mM solution in DMSO (Cat. No. 508340).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Perk
Reversible: yes
Target IC50: 0.4 nM against EIF2AK3/PERK-catalyzed EIF2&alpha

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

2024 CiteAb Award Winner for Supplier Succeeding in Parkinson′s Research

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Bibha Dahal et al.
Virology, 539, 121-128 (2019-11-17)
Venezuelan equine encephalitis virus (VEEV) is a neurotropic virus that causes significant disease in both humans and equines. Here we characterized the impact of VEEV on signaling pathways regulating cell death in human primary astrocytes. VEEV productively infected primary astrocytes
Jessica Proulx et al.
Frontiers in neuroscience, 16, 906651-906651 (2022-07-06)
Astrocytes are one of the most numerous glial cells in the central nervous system (CNS) and provide essential support to neurons to ensure CNS health and function. During a neuropathological challenge, such as during human immunodeficiency virus (HIV)-1 infection or
Alba Corman et al.
PLoS biology, 19(5), e3001263-e3001263 (2021-05-26)
We here conducted an image-based chemical screen to evaluate how medically approved drugs, as well as drugs that are currently under development, influence overall translation levels. None of the compounds up-regulated translation, which could be due to the screen being

Global Trade Item Number

SKUGTIN
516535-5MG04055977198126