Product Name :
GSK2656157
Description:
GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC50 of 0.9 nM. It is highly selective for PERK with IC50 values >100 nM against a panel of 300 kinases. GSK2656157 inhibits PERK activity in cells with an IC50 in the range of 10-30 nM as shown by inhibition of stress-induced PERK autophosphorylation, eIF2α substrate phosphorylation, together with corresponding decreases in ATF4 and CHOP proteins in multiple cell lines. Oral administration of GSK2656157 to mice shows a dose- and time-dependent pharmacodynamic response in pancreas as measured by PERK auto-phosphorylation.
CAS:
1337532-29-2
Molecular Weight:
416.45
Formula:
C23H21FN6O
Chemical Name:
1-(5-{4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl}-4-fluoro-2,3-dihydro-1H-indol-1-yl)-2-(6-methylpyridin-2-yl)ethan-1-one
Smiles :
CN1C=C(C2=C1N=CN=C2N)C1=CC=C2C(CCN2C(=O)CC2=CC=CC(C)=N2)=C1F
InChiKey:
PRWSIEBRGXYXAJ-UHFFFAOYSA-N
InChi :
InChI=1S/C23H21FN6O/c1-13-4-3-5-14(28-13)10-19(31)30-9-8-16-18(30)7-6-15(21(16)24)17-11-29(2)23-20(17)22(25)26-12-27-23/h3-7,11-12H,8-10H2,1-2H3,(H2,25,26,27)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Puromycin aminonucleoside} site|{Puromycin aminonucleoside} Apoptosis|{Puromycin aminonucleoside} Epigenetics|{Puromycin aminonucleoside} Protocol|{Puromycin aminonucleoside} Data Sheet|{Puromycin aminonucleoside} supplier}
Shelf Life:
≥360 days if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC50 of 0.{{Omburtamab} web|{Omburtamab} Immunology/Inflammation|{Omburtamab} Biological Activity|{Omburtamab} In Vitro|{Omburtamab} manufacturer|{Omburtamab} Epigenetic Reader Domain} 9 nM.PMID:27217159 It is highly selective for PERK with IC50 values >100 nM against a panel of 300 kinases. GSK2656157 inhibits PERK activity in cells with an IC50 in the range of 10-30 nM as shown by inhibition of stress-induced PERK autophosphorylation, eIF2α substrate phosphorylation, together with corresponding decreases in ATF4 and CHOP proteins in multiple cell lines. Oral administration of GSK2656157 to mice shows a dose- and time-dependent pharmacodynamic response in pancreas as measured by PERK auto-phosphorylation.|Product information|CAS Number: 1337532-29-2|Molecular Weight: 416.45|Formula: C23H21FN6O|Chemical Name: 1-(5-{4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl}-4-fluoro-2,3-dihydro-1H-indol-1-yl)-2-(6-methylpyridin-2-yl)ethan-1-one|Smiles: CN1C=C(C2=C1N=CN=C2N)C1=CC=C2C(CCN2C(=O)CC2=CC=CC(C)=N2)=C1F|InChiKey: PRWSIEBRGXYXAJ-UHFFFAOYSA-N|InChi: InChI=1S/C23H21FN6O/c1-13-4-3-5-14(28-13)10-19(31)30-9-8-16-18(30)7-6-15(21(16)24)17-11-29(2)23-20(17)22(25)26-12-27-23/h3-7,11-12H,8-10H2,1-2H3,(H2,25,26,27)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥360 days if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|