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

1 Citations COA COA
In stock
Item Number
G125654
Grouped product items
SKU Size
Availability
 Price Qty
G125654-5mg
5mg
3
$89.90
G125654-25mg
25mg
3
$299.90
G125654-100mg
100mg
2
$640.90
G125654-500mg
500mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,922.90
Wish List
Bulk Order  SDS  DATASHEET  Specification Sheet

Potent and selective PERK inhibitor

View related series
Apoptosis (4276) Autophagy (1917) Cell Cycle/DNA Damage (2602) PERK (19) Unfolded Protein Response (214)

Basic Description

Synonyms AC-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 Moligand™, ≥98%
Biochemical and Physiological Mechanisms Potent 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 Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
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.

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Indoles and derivatives
Subclass Phenylacetylindoles
Intermediate Tree Nodes Not available
Direct Parent Phenylacetylindoles
Alternative Parents Trifluoromethylbenzenes  Phenylacetamides  Indoles  Pyrrolo[2,3-d]pyrimidines  Aminopyrimidines and derivatives  N-methylpyrroles  Imidolactams  Tertiary carboxylic acid amides  Heteroaromatic compounds  Amino acids and derivatives  Azacyclic compounds  Organofluorides  Organic oxides  Alkyl fluorides  Hydrocarbon derivatives  Carbonyl compounds  Primary amines  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Phenylacetylindole - Trifluoromethylbenzene - Phenylacetamide - Pyrrolo[2,3-d]pyrimidine - Indole - Pyrrolopyrimidine - Aminopyrimidine - Monocyclic benzene moiety - N-methylpyrrole - Imidolactam - Benzenoid - Substituted pyrrole - Pyrimidine - Heteroaromatic compound - Tertiary carboxylic acid amide - Pyrrole - Amino acid or derivatives - Carboxamide group - Carboxylic acid derivative - Azacycle - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Hydrocarbon derivative - Organic oxide - Alkyl halide - Carbonyl group - Organic oxygen compound - Organic nitrogen compound - Alkyl fluoride - Amine - Primary amine - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as phenylacetylindoles. These are compounds containing an indole moiety attached to phenylacetate derivative.
External Descriptors Not available

Associated Targets(Human)

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

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Toxoplasma gondii (4585 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Canis familiaris (36305 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MEF (1005 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
L929 (3802 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

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)
InChIKey SIXVRXARNAVBTC-UHFFFAOYSA-N
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
Molecular Weight 451.44
Reaxy-Rn 21981831
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21981831&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

6 results found

Lot Number Certificate Type Date Item
G2503350 Certificate of Analysis May 17, 2025 G125654
G2503375 Certificate of Analysis May 17, 2025 G125654
G2503392 Certificate of Analysis May 17, 2025 G125654
G2503393 Certificate of Analysis May 17, 2025 G125654
L2322055 Certificate of Analysis Jan 02, 2024 G125654
K1630020 Certificate of Analysis Jun 17, 2022 G125654

Chemical and Physical Properties

Solubility Solvent:DMSO, Max Conc. mg/mL: 45.14, Max Conc. mM: 100
Molecular Weight 451.400 g/mol
XLogP3 3.800
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 3
Exact Mass 451.162 Da
Monoisotopic Mass 451.162 Da
Topological Polar Surface Area 77.000 Ų
Heavy Atom Count 33
Formal Charge 0
Complexity 721.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Citations of This Product

How to Cite Aladdin Scientific Products?
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). 

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