GSK2656157 化学構造
分子量: 416.45





  • Compare PERK Inhibitors



製品説明 GSK2656157は一種のATP競争性的で、高度選択性的なPERK阻害剤で、無細胞試験でIC50値が0.9 nMですが、PERKに作用する選択性は一組の300種キナーゼに作用する選択性より500倍余りが高くなります。



0.9 nM [1]

In vitro試験 Pretreatment of cells with GSK2656157 results in inhibition of PERK activation as well as decreases in the downstream substrates, phospho-eIF2a, ATF4, and CHOP with an IC50 in the range of 10-30 nM. Cells that are exposed to 1 mM GSK2656157 before UPR induction are able to block this effect on de novo protein synthesis. Five of 84 UPR-related genes (DDIT3, HERPUD1, PPP1R15A, C/EBP-beta, and ERN1) are down regulated more than 4-fold by GSK2656157. 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. Thus, GSK2656157 can be used to evaluate the biologic function of PERK in various biologic contexts. [1]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
human A549 cells M3\6S2Z2dmO2aX;uJIF{e2G7 M1rWclEhcA>? NYntdHh5UW6qaXLpeIlwdiCxZjD0bIFxe2mpYYLnbY4ucW6mdXPl[EBifXSxcHjvd5Bpd3K7bHH0bY9vKG:oIGDFVmshcW5iaIXtZY4hSTV2OTDj[YxteyCycnXpcoN2[mG2ZXSg[o9zKDFiaIKg[o9tdG:5ZXSgZpkhfGijcIPp[4Fz\2mwLXnu[JVkfGmxbjDt[YF{fXKnZDDh[pRmeiBzIHjyJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZMtKEmFNUC9NE4xOyEQvF2= NX\1PIJvOjR7MEC1PVM>

... Click to View More Cell Line Experimental Data

In vivo試験 Complete inhibition of phospho-PERK Thr980 is observed through 8 hours after a single 50 mg/kg oral dose of GSK2656157. Treatment of mice with 50 or 150 mg/kg twice daily dosing of GSK2656157 results in dose-dependent inhibition of tumor growth in four models; reaching 54–114% tumor growth inhibition at the 150 mg/kg, twice daily dose. Altered amino acid metabolism, decreased blood vessel density, and vascular perfusion are potential mechanisms for the observed antitumor effect. Treatment of mice with GSK2656157 results in inhibition of tumor growth in multiple human tumor xenografts. [1]
特集 Orally bioavailable PERK-selective inhibitor that functions independent of eIF2α phosphorylation.

プロトコル (参考用のみ)



Kinase assay Inhibitory potency of GSK2656157 is measured using recombinant GST-PERK (536–1116 amino acids) with 6-His-full-length human eIF2a as a substrate. Kinase selectivity is evaluated using 27 kinases at GSK as well as a panel of 300 kinases.



細胞株 human tumor cell lines, primary human microvascular endothelial cells
濃度 ~3 μM
反応時間 3 day

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.



動物モデル human tumor xenograft models
製剤 0.5% hydroxypropyl methyl cellulose, 0.1% tween-80 in water (pH 6.75).
投薬量 50 or 150 mg/kg, twice daily
投与方法 Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download GSK2656157 SDF
分子量 416.45


CAS No. 1337532-29-2
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 32 mg/mL (76.83 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyridin-2-yl)ethanone

文献中の引用 (5)



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


* 必須

Related PERK 阻害剤


Tags: GSK2656157を買う | GSK2656157供給者 | GSK2656157を購入する | GSK2656157費用 | GSK2656157生産者 | オーダーGSK2656157 | GSK2656157代理店
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID