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GSK1059615 - ≥98%, high purity , PI3-kinase class I inhibitor, CAS No.958852-01-2, PI3-kinase class I inhibitor

COA COA
In stock
Item Number
G127955
Grouped product items
SKU Size
Availability
 Price Qty
G127955-5mg
5mg
3
$75.90
G127955-25mg
25mg
3
$342.90
G127955-100mg
100mg
2
$706.90
Wish List
Bulk Order  SDS  DATASHEET  Specification Sheet

Potent PI 3-kinase inhibitor

View related series
Apoptosis (4276) mTOR (145) phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit alpha Inhibitor (76) PI3K (243) PI3K/Akt/mTOR (765)

Basic Description

Synonyms Thiodiphenylamin [German] | D70652 | OXIRANE,2-[(PHENYLMETHOXY)METHYL]- | BRD-K06750613-001-01-6 | HY-12036 | NCGC00346509-02 | (Z)-5-((4-(pyridin-4-yl)quinolin-6-yl)methylene)thiazolidine-2,4-dione | GSK 1059615 sodium salt hydrate | GSK1059615 | GSK-105
Specifications & Purity Moligand™, ≥98%
Biochemical and Physiological Mechanisms Potent inhibitor of PI 3-kinaseα(PI3Kα) (IC50= 2 nM). Inhibits proliferation in BT474 cells and attenuates MAPK signaling.
Storage Temp Store at 2-8°C
Shipped In
Wet ice
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action PI3-kinase class I inhibitor
Product Description

GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
A potent inhibitor of PI 3-kinase and FRAP (mTOR)

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Pyridines and derivatives
Subclass Bipyridines and oligopyridines
Intermediate Tree Nodes Not available
Direct Parent Bipyridines and oligopyridines
Alternative Parents Quinolines and derivatives  Thiazolidinediones  Benzenoids  Heteroaromatic compounds  Dicarboximides  Thiocarbamic acid derivatives  Azacyclic compounds  Organonitrogen compounds  Organic oxides  Hydrocarbon derivatives  Carbonyl compounds  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Bipyridine - Quinoline - Thiazolidinedione - Benzenoid - Dicarboximide - Thiazolidine - Heteroaromatic compound - Thiocarbamic acid derivative - Carboxylic acid derivative - Azacycle - Organic nitrogen compound - Organic oxide - Organic oxygen compound - Organooxygen compound - Organonitrogen compound - Hydrocarbon derivative - Carbonyl group - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as bipyridines and oligopyridines. These are organic compounds containing two pyridine rings linked to each other.
External Descriptors Not available

Product Properties

ALogP 3

Associated Targets(Human)

CSNK2A2 Tchem Casein kinase II subunit alpha' (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
TAOK1 Tchem Serine/threonine-protein kinase TAO1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PIK3CA Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
Tchem Uncharacterized protein FLJ45252 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CLK1 Tchem Dual specificity protein kinase CLK1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CLK2 Tchem Dual specificity protein kinase CLK2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TOP2A Tclin DNA topoisomerase II alpha (6317 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDGFRB Tclin Platelet-derived growth factor receptor beta (5195 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KIT Tclin Stem cell growth factor receptor (10667 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DCK Tchem Deoxycytidine kinase (530 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK11 Tchem MAP kinase p38 beta (2785 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
NQO2 Tchem Quinone reductase 2 (885 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKACB Tchem cAMP-dependent protein kinase beta-1 catalytic subunit (589 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCZ Tchem Protein kinase C zeta (2414 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K6 Tchem Dual specificity mitogen-activated protein kinase kinase 6 (1284 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MYLK Tchem Myosin light chain kinase, smooth muscle (1267 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1G1 Tchem Casein kinase I gamma 1 (2496 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FGFR1 Tclin Fibroblast growth factor receptor 1 (9149 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
STK3 Tchem Serine/threonine-protein kinase MST2 (3069 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKAG1 Tchem AMP-activated protein kinase, gamma-1 subunit (254 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K5 Tchem Dual specificity mitogen-activated protein kinase kinase 5 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K3 Tchem Dual specificity mitogen-activated protein kinase kinase 3 (632 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK6 Tclin Cyclin-dependent kinase 6 (1724 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKAG2 Tchem AMP-activated protein kinase, gamma-2 subunit (243 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AKT2 Tchem Serine/threonine-protein kinase AKT2 (4301 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AKT3 Tchem Serine/threonine-protein kinase AKT3 (3157 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GRK2 Tchem G-protein coupled receptor kinase 2 (1019 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PYGB Tchem Brain glycogen phosphorylase (474 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
RPS6KA4 Tchem Ribosomal protein S6 kinase alpha 4 (2104 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ROCK1 Tclin Rho-associated protein kinase 1 (4723 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIM1 Tchem Serine/threonine-protein kinase PIM1 (9629 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PKN2 Tchem Protein kinase N2 (1991 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSK Tchem Tyrosine-protein kinase CSK (2395 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKD3 Tchem Protein kinase C nu (2315 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCI Tchem Protein kinase C iota (2821 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SYK Tclin Tyrosine-protein kinase SYK (7372 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PLK1 Tchem Serine/threonine-protein kinase PLK1 (28605 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
JAK1 Tclin Tyrosine-protein kinase JAK1 (8569 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha 1 (2796 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA6 Tchem Ribosomal protein S6 kinase alpha 6 (2027 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PFKP Tbio Phosphofructokinase platelet type (224 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1E Tclin Casein kinase I epsilon (1412 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CAMK4 Tbio CaM kinase IV (2116 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3A Tclin Glycogen synthase kinase-3 alpha (3764 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Cdk4 Cyclin-dependent kinase 4 (3 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Pygl Liver glycogen phosphorylase (81 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Prkcd Protein kinase C delta (192 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Prkcb Protein kinase C beta (2 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Camk2g CaM kinase II gamma (1 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Tec Tyrosine-protein kinase TEC (25 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AIRC Multifunctional protein ADE2 (8 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
Septin9 Septin-9 (1 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Acadvl Very long-chain specific acyl-CoA dehydrogenase, mitochondrial (1 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

Pubchem Sid 488200355
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/488200355
IUPAC Name (5Z)-5-[(4-pyridin-4-ylquinolin-6-yl)methylidene]-1,3-thiazolidine-2,4-dione
INCHI InChI=1S/C18H11N3O2S/c22-17-16(24-18(23)21-17)10-11-1-2-15-14(9-11)13(5-8-20-15)12-3-6-19-7-4-12/h1-10H,(H,21,22,23)/b16-10-
InChIKey QDITZBLZQQZVEE-YBEGLDIGSA-N
Smiles C1=CC2=NC=CC(=C2C=C1C=C3C(=O)NC(=O)S3)C4=CC=NC=C4
Isomeric SMILES C1=CC2=NC=CC(=C2C=C1/C=C\3/C(=O)NC(=O)S3)C4=CC=NC=C4
Molecular Weight 333.36
Reaxy-Rn 20875363
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20875363&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.

8 results found

Lot Number Certificate Type Date Item
C2316756 Certificate of Analysis Dec 13, 2024 G127955
C2316754 Certificate of Analysis Dec 13, 2024 G127955
C2316753 Certificate of Analysis Dec 13, 2024 G127955
C2316751 Certificate of Analysis Dec 05, 2024 G127955
C2316762 Certificate of Analysis Dec 05, 2024 G127955
C2316755 Certificate of Analysis Dec 05, 2024 G127955
C2313756 Certificate of Analysis Dec 09, 2022 G127955
C2313754 Certificate of Analysis Dec 09, 2022 G127955

Chemical and Physical Properties

Solubility Solvent:DMSO, Max Conc. mg/mL: 3.33, Max Conc. mM: 10
Refractive Index 1.76
Molecular Weight 333.400 g/mol
XLogP3 3.000
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 5
Rotatable Bond Count 2
Exact Mass 333.057 Da
Monoisotopic Mass 333.057 Da
Topological Polar Surface Area 97.300 Ų
Heavy Atom Count 24
Formal Charge 0
Complexity 544.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 1
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 1
Covalently-Bonded Unit Count 1

Solution Calculators

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