GSK2656157

SKU: orb1305213

Description

GSK2656157 is a potent and highly selective ATP-competitive inhibitor of PERK, demonstrating an IC50 of 0.9 nM in biochemical assays with over 500-fold selectivity across 300 kinases. This tool compound is widely used in vitro and in vivo to investigate the unfolded protein response, ER stress signaling, and related pathologies such as cancer and neurodegenerative diseases.

Research Area

Cell Biology

Images & Validation

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Key Properties

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CAS Number	1337532-29-2
MW	416.45
Purity	>99.99% (May vary between batches)
Formula	C₂₃H₂₁FN₆O
SMILES	Cc1cccc(CC(=O)N2CCc3c2ccc(-c2cn(C)c4ncnc(N)c24)c3F)n1
Target	Apoptosis,Autophagy,PERK
Solubility	DMSO:13.89 mg/mL (33.35 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween-80+45% Saline:0.5 mg/mL (1.2 mM)

Bioactivity

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Target IC50	EIF2AK2 (PKR):905 nM\|WNK3:5951 nM\|c-MER:3431 nM\|BRK:905 nM\|EIF2AK1 (HRI):460 nM\|LRRK2:6918 nM\|EIF2AK4(GCN2):3162 nM\|NEK1:9807 nM\|MLK2:2796 nM\|AXL:9808 nM\|JAK2:24547 nM\|MSK1:8985 nM\|MEKK3:954 nM\|MEKK3:2847 nM\|Aurora B:1259 nM\|KHS:1764 nM\|PI3Kγ:3802 nM\|LCK:2344 nM\|MLCK2:3039 nM\|ROCK1:7244 nM\|ALK5:3020 nM\|PERK:0.9 nM Read more...
In Vivo	GSK2656157 (1 mM) can induce the unfolded protein response (UPR) and inhibit de novo protein synthesis. It downregulates 6% of UPR-related genes (PPP1R15A, HERPUD1, DDIT3, C/EBP-β, and ERN1), with a reduction exceeding fourfold for these targets. Pre-treatment with GSK2656157 inhibits PERK activation and decreases downstream substrates, including phospho-eIF2a, ATF4, and CHOP (IC50: 10-30 nM). In the absence of exogenous UPR inducers, GSK2656157 does not affect cell growth (IC50: 6-25 mM). Read more...
In Vitro	GSK2656157 inhibits the growth of various human xenograft tumors in mice. Administered at a dose of 50 mg/kg orally, GSK2656157 completely suppresses phospho-PERK Thr980 after 8 hours. Furthermore, with dosages of 50/150 mg/kg administered twice daily, GSK2656157 exhibits a dose-dependent suppression of tumor growth in four different mouse cancer models, achieving a 54-114% inhibition of tumor growth at 150 mg/kg. Read more...
Cell Research	Antiproliferative activity of GSK2656157 against multiple human tumor cell lines as well as primary human microvascular endothelial cells is evaluated in a 3-day proliferation assay using standard culture medium. In the absence of exogeneous UPR inducers, GSK2656157 has no significant effect on the growth of any of these cells with IC50 range of 6–25 mM. (Only for Reference) Read more...

Storage & Handling

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Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Autophagy, Apoptosis, Inhibitor, GSK2656157, GSK-2656157, GSK 2656157, inhibit, PERK, Protein kinase R-like endoplasmic reticulum kinase, PKR-like endoplasmic reticulum kinase

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Compound Identifiers

PubChem CID

53469059 ↗

Key Properties

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No computed properties available.

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GSK2656157 (orb1305213)

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Purity:	>98% (HPLC)
CAS Number:	1337532-29-2
MW:	416.45
Formula:	C₂₃H₂₁FN₆O

GSK2656157

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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