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5.04651

GSK2656157

≥98% (HPLC), powder, PERK inhibitor, Calbiochem®

Synonym(s):

PERK Inhibitor II, GSK2656157, BRK Inhibitor II, EIF2AK1 Inhibitor II, EIF2AK2 Inhibitor III, EIF2AK3 Inhibitor II, HRI Inhibitor II, MEKK2 Inhibitor I, PKR Inhibitor III, PKR-like ER Kinase Inhibitor II

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Size/SKUAvailabilityPrice
5 mg
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$230.00

About This Item

Empirical Formula (Hill Notation):
C23H21FN6O
CAS Number:
1337532-29-2
Molecular Weight:
416.45
MDL number:
MFCD27997885
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light

$230.00

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Product Name

PERK Inhibitor II, GSK2656157,

assay

≥98% (HPLC)

Quality Segment

100

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 100 mg/mL

storage temp.

−20°C

SMILES string

Fc1c2c(ccc1c4c5c([n](c4)C)ncnc5N)N(CC2)C(=O)Cc3nc(ccc3)C

InChI key

PRWSIEBRGXYXAJ-UHFFFAOYSA-N

General description

A cell-permeable pyrrolopyrimidinamine compound that acts as a potent, ATP-competitive EIF2AK3/PERK inhibitor (IC50 = 0.9 nM; [ATP] = 10 µM), displaying ≥511-fold selectivity over HRI/EIF2AK1, BRK, PKR/EIF2AK2, and MEKK2 (IC50 = 460, 822, 905, and 954 nM, respectively) and much reduced or little activity toward more than 300 other kinases. While GSK2656157 potently inhibits ER stress-induced enhancement of PERK and eIF2α phosphorylation as well as ATF4 & CHOP upregulation in human PxBC3 and murine LL/2 cultures in vitro (IC50 ≤30 nM; 1 h drug preincubation prior to 6 h ER-stress induction by 1 µM Thapsigargin, only basal PERK phosphorylation, but not basal eIF2α phosphorylation or ATF4 & CHOP expression, is seen inhibited in pancreas (by >95% up to 8 h post single 50 mg/kg oral dose) and tumor tissues upon GSK2656157 administration in mice in vivo, resulting in the observed antitumor efficacy (54-110% tumor growth inhibition; 150 mg/kg/12 h via p.o.) and reversible pancreas damage (44% and 95% of control pancreas mass, respectively, 1 d and 15 d post 14 d 150 mg/kg/12 h oral dosing). Comparing to its structural analog GSK2606414 (Cat. No. 516535), GSK2656157 exhibits much reduced potency toward Aurora B, MLK2/MAP3K10, MLCK2/MYLK2, c-MER (IC50 = 1.259, 2.796, 3.039, and 3.431 µM, respectively), c-Kit, and DDR2 (69.84% and 25.41% inhibition, respectively, at 10 µM)

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PERK
Reversible: yes

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.
Use only fresh DMSO for reconstitution.

Other Notes

Atkins, C., et al. 2013. Cancer Res.73, 1993.

Legal Information

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

Disclaimer

Toxicity: Regulatory Review (Z)

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This Item
516535509522530758
PERK Inhibitor II, GSK2656157

Sigma-Aldrich

504651

PERK Inhibitor II, GSK2656157

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

Transglutaminase 2 Inhibitor II, ERW1041E

Sigma-Aldrich

509522

Transglutaminase 2 Inhibitor II, ERW1041E

BMX/BTK Inhibitor II, QL47

Sigma-Aldrich

530758

BMX/BTK Inhibitor II, QL47

description

-

description

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.

description

-

description

-

assay

≥98% (HPLC)

assay

≥99% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

form

powder

form

solid

form

powder

Quality Level

100

Quality Level

200

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

solubility

DMSO: 100 mg/mL

solubility

DMSO: 100 mg/mL

solubility

DMSO: 100 mg/mL

solubility

glacial acetic acid: 2 mg/mL

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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