GSK2606414 - ≥98%, high purity , CAS No.1337531-36-8

1 Citations
  • ≥98%
Item Number
G125654
Grouped product items
SKUSizeAvailabilityPrice Qty
G125654-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$116.90
G125654-25mg
25mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$526.90
G125654-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$640.90

Potent and selective PERK inhibitor

Basic Description

SynonymsAC-29016 | 1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone | Ethanone, 1-(5-(4-amino-7-methyl-7H-pyrrolo(2,3-d)pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl)-2-(3-(trifluoromethyl)phenyl)- | 1-[5-(4-a
Specifications & Purity≥98%
Biochemical and Physiological MechanismsPotent and selective protein kinase R-like ER kinase (PERK) inhibitor (IC50= 0.4 nM). Exhibits >1000-fold selectivity for PERK over HR1 and PKR. Inhibits thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells. Attenuates subcutaneous pancr
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Note卖完停产,不再备货
Product Description

GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed.

Associated Targets(Human)

CYP2C8 Tchem Cytochrome P450 2C8 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EIF2AK3 Tchem Eukaryotic translation initiation factor 2-alpha kinase 3 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RIPK1 Tchem Receptor-interacting serine/threonine-protein kinase 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KIT Tclin Stem cell growth factor receptor (10667 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C8 Tchem Cytochrome P450 2C8 (1492 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKB Tchem Serine/threonine-protein kinase Aurora-B (6805 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP3K11 Tchem Mitogen-activated protein kinase kinase kinase 11 (808 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP3K10 Tchem Mitogen-activated protein kinase kinase kinase 10 (401 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NTRK1 Tclin Nerve growth factor receptor Trk-A (7922 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MYLK2 Tchem myosin light chain kinase 2 (424 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP3K9 Tchem Mitogen-activated protein kinase kinase kinase 9 (945 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
IKBKE Tchem Inhibitor of nuclear factor kappa B kinase epsilon subunit (3311 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
YES1 Tclin Tyrosine-protein kinase YES (2781 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK2 Tchem Serine/threonine-protein kinase NEK2 (3514 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTK6 Tchem Tyrosine-protein kinase BRK (2605 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK9 Tchem Serine/threonine-protein kinase NEK9 (1479 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK6 Tchem Serine/threonine-protein kinase NEK6 (1986 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP4K5 Tchem Mitogen-activated protein kinase kinase kinase kinase 5 (1523 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BXPC-3 (2997 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Caco-2 (12174 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RET Tclin Tyrosine-protein kinase receptor RET (6732 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AXL Tchem Tyrosine-protein kinase receptor UFO (3469 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NTRK2 Tclin Neurotrophic tyrosine kinase receptor type 2 (3279 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK7 Tchem Serine/threonine-protein kinase NEK7 (1804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MERTK Tchem Proto-oncogene tyrosine-protein kinase MER (2687 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RIPK1 Tchem Receptor-interacting serine/threonine-protein kinase 1 (1548 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NTRK3 Tclin NT-3 growth factor receptor (2338 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK5 Tchem Serine/threonine-protein kinase Nek5 (349 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DDR2 Tchem Discoidin domain-containing receptor 2 (2199 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EIF2AK2 Tchem Interferon-induced, double-stranded RNA-activated protein kinase (504 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK4 Tchem Serine/threonine-protein kinase Nek4 (980 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK1 Tchem Serine/threonine-protein kinase Nek1 (1886 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK3 Tchem Serine/threonine-protein kinase Nek3 (902 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK11 Tchem Serine/threonine-protein kinase Nek11 (645 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
WNK2 Tchem Serine/threonine-protein kinase WNK2 (570 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EIF2AK1 Tchem Eukaryotic translation initiation factor 2-alpha kinase 1 (688 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EIF2AK3 Tchem Eukaryotic translation initiation factor 2-alpha kinase 3 (635 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK10 Tchem Serine/threonine-protein kinase Nek10 (176 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Toxoplasma gondii (4585 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Canis familiaris (36305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MEF (1005 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
L929 (3802 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 1-[5-(4-amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethanone
INCHI InChI=1S/C24H20F3N5O/c1-31-12-18(21-22(28)29-13-30-23(21)31)15-5-6-19-16(11-15)7-8-32(19)20(33)10-14-3-2-4-17(9-14)24(25,26)27/h2-6,9,11-13H,7-8,10H2,1H3,(H2,28,29,30)
InChi Key SIXVRXARNAVBTC-UHFFFAOYSA-N
Canonical SMILES CN1C=C(C2=C(N=CN=C21)N)C3=CC4=C(C=C3)N(CC4)C(=O)CC5=CC(=CC=C5)C(F)(F)F
Isomeric SMILES CN1C=C(C2=C(N=CN=C21)N)C3=CC4=C(C=C3)N(CC4)C(=O)CC5=CC(=CC=C5)C(F)(F)F
PubChem CID 53469448
Molecular Weight 451.44

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

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2 results found

Lot NumberCertificate TypeDateItem
L2322055Certificate of AnalysisJan 02, 2024 G125654
K1630020Certificate of AnalysisJun 17, 2022 G125654

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 45.14, Max Conc. mM: 100

Related Documents

Citations of This Product

1. Xiaohua Xie, Xiaofeng Wu, Dongsheng Zhao, Ying Liu, Qiyue Du, Yitian Li, Yaping Xu, Yuhang Li, Yan Qiu, Yungang Yang.  (2023)  Fluvoxamine alleviates bleomycin-induced lung fibrosis via regulating the cGAS-STING pathway.  PHARMACOLOGICAL RESEARCH,  187  (106577).  [PMID:36435270]

References

1. Xiaohua Xie, Xiaofeng Wu, Dongsheng Zhao, Ying Liu, Qiyue Du, Yitian Li, Yaping Xu, Yuhang Li, Yan Qiu, Yungang Yang.  (2023)  Fluvoxamine alleviates bleomycin-induced lung fibrosis via regulating the cGAS-STING pathway.  PHARMACOLOGICAL RESEARCH,  187  (106577).  [PMID:36435270]

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