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Merck

516535

GSK2606414

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

Synonym(s):

PERK Inhibitor I, GSK2606414

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5 MG

CZK 5,030.00

CZK 5,030.00

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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

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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.

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

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

Quality Level

200

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1 of 4

This Item
218719528245372040
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.

Sigma-Aldrich

516535

PERK Inhibitor I, GSK2606414

Casein Kinase I Inhibitor III, PF-4800567 The Casein Kinase I Inhibitor III, PF-4800567 controls the biological activity of Casein Kinase I. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sigma-Aldrich

218719

Casein Kinase I Inhibitor III, PF-4800567

PLD Inhibitor, FIPI The PLD Inhibitor, FIPI controls the biological activity of PLD. This small molecule/inhibitor is primarily used for Membrane applications.

Sigma-Aldrich

528245

PLD Inhibitor, FIPI

Haspin Kinase Inhibitor, CHR-6494

Sigma-Aldrich

372040

Haspin Kinase Inhibitor, CHR-6494

assay

≥99% (HPLC)

assay

≥99% (HPLC)

assay

≥99% (HPLC)

assay

≥98% (HPLC)

form

powder

form

solid

form

powder

form

solid

Quality Level

200

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

Disclaimer

Toxicity: Standard Handling (A)

Biochem/physiol Actions

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

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).

Other Notes

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

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.

Legal Information

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

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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