10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
GSK621 GSK621 is a specific and potent AMPK activator.
Targets
AMPK (Cell-free assay)
In vitro
In AML cell lines and primary AML samples, GSK621 markedly increases phosphorylation at AMPKα T172, a marker of AMPK activation. In a set of 20 cell lines, GSK621 reduces the proliferation of all 20 lines with IC50 ranged from 13-30 μM, and increases apoptosis in 17 (85%) lines. In addition, GSK621 also triggers autophagy, which partially contributes to AML cell death.
In vivo
In nude mice bearing MOLM-14 xenografts, GSK621 (30 mg/kg, i.p.) reduces leukemia growth and significantly extends survival by enhancing AMPK activity and the induction of apoptosis.
Cell Research(from reference)
Cell lines：MV4-11, OCI-AML3, OCI-AML2, HL-60, Kasumi, HEL, UT7, NB4, TF-1, KG1A, Nomo p28, SKM-1, U937, YHP1, MOLM-14, Mo7e, K562, MOLM-13, EOL-1, SET-2 cell lines
Concentrations：~30 μM
Incubation Time：~4 d
| Canonical Smiles | COC1=CC=CC(=C1)N2C(=O)C3=C(C=C(N3C4=CC=C(C=C4)C5=C(C(=CC=C5)OC)O)Cl)NC2=O |
|---|---|
| IUPAC Name | 6-chloro-5-[4-(2-hydroxy-3-methoxyphenyl)phenyl]-3-(3-methoxyphenyl)-1H-pyrrolo[3,2-d]pyrimidine-2,4-dione |
| InChIKey | KURYSXLJGKKDHT-UHFFFAOYSA-N |
| INCHI | 1S/C26H20ClN3O5/c1-34-18-6-3-5-17(13-18)30-25(32)23-20(28-26(30)33)14-22(27)29(23)16-11-9-15(10-12-16)19-7-4-8-21(35-2)24(19)31/h3-14,31H,1-2H3,(H,28,33) |
| Isomeric SMILES | COC1=CC=CC(=C1)N2C(=O)C3=C(C=C(N3C4=CC=C(C=C4)C5=C(C(=CC=C5)OC)O)Cl)NC2=O |
| Molecular Weight | 489.91 |
| Reaxy-Rn | 22062809 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=22062809&ln= |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Class | Pyrroles |
| Subclass | Substituted pyrroles |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Phenylpyrroles |
| Alternative Parents | Methoxyphenols Alpha amino acids and derivatives Pyrrolopyrimidines Phenoxy compounds Methoxybenzenes Anisoles Pyrimidones Alkyl aryl ethers 1-hydroxy-4-unsubstituted benzenoids N-acyl amines Hydropyrimidines Vinylogous amides Heteroaromatic compounds Dicarboximides Trialkylamines Organic carbonic acids and derivatives Lactams Vinyl chlorides Enamines Chloroalkenes Azacyclic compounds Organopnictogen compounds Organochlorides Organic oxides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | 1-phenylpyrrole - Methoxyphenol - Alpha-amino acid or derivatives - Pyrrolopyrimidine - Phenoxy compound - Methoxybenzene - Phenol ether - Anisole - 1-hydroxy-4-unsubstituted benzenoid - Pyrimidone - Phenol - Alkyl aryl ether - Benzenoid - Pyrimidine - N-acyl-amine - 1,2,3,4-tetrahydropyrimidine - Hydropyrimidine - Monocyclic benzene moiety - Heteroaromatic compound - Vinylogous amide - Dicarboximide - Tertiary aliphatic amine - Tertiary amine - Carbonic acid derivative - Lactam - Amino acid or derivatives - Azacycle - Chloroalkene - Haloalkene - Vinyl halide - Vinyl chloride - Ether - Enamine - Carboxylic acid derivative - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Organochloride - Organohalogen compound - Amine - Aromatic heteropolycyclic compound |
| Description | This compound belongs to the class of organic compounds known as phenylpyrroles. These are polycyclic aromatic compounds containing a benzene ring linked to a pyrrole ring through a CC or CN bond. |
| External Descriptors | Not available |
| Molecular Weight | 489.900 g/mol |
|---|---|
| XLogP3 | 5.100 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 5 |
| Rotatable Bond Count | 5 |
| Exact Mass | 489.109 Da |
| Monoisotopic Mass | 489.109 Da |
| Topological Polar Surface Area | 93.000 Ų |
| Heavy Atom Count | 35 |
| Formal Charge | 0 |
| Complexity | 778.000 |
| 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 |
