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GSK2334470 - 95%, high purity , CAS No.1227911-45-6, Inhibitor of 3-phosphoinositide dependent protein kinase 1;Inhibitor of aurora kinase A;Inhibitor of aurora kinase B

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Item Number
G126481
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G126481-5mg
5mg
4
$58.90
G126481-10mg
10mg
3
$97.90
G126481-25mg
25mg
1
$220.90
G126481-50mg
50mg
1
$325.90
G126481-100mg
100mg
1
$543.90
G126481-200mg
200mg
1
$979.90

Novel, potent PDK1 inhibitor

Basic Description

Synonyms AKOS024458000 | Q27077885 | (3S,6R)-1-(6-(3-amino-1H-indazol-6-yl)-2-(methylamino)pyrimidin-4-yl)-N-cyclohexyl-6-methylpiperidine-3-carboxamide | 3-Piperidinecarboxamide, 1-[6-(3-amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-
Specifications & Purity Moligand™, ≥95%
Biochemical and Physiological Mechanisms GSK2334470 is a highly specific and potent inhibitor of PDK1 (3-Phosphoinositide dependent protein kinase-1). GSK2334470 can be used in cells to ablate T-loop phosphorylation and activate SGK, S6K1 and RSK as well as suppress the activation of Akt.Novel,
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™
Action Type INHIBITOR
Mechanism of action Inhibitor of 3-phosphoinositide dependent protein kinase 1;Inhibitor of aurora kinase A;Inhibitor of aurora kinase B
Note Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM, with no activity at other close related AGC-kinases.
A potent and selective PDK1 inhibitor that subsequently induces apoptotic cell death

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Benzopyrazoles
Subclass Indazoles
Intermediate Tree Nodes Not available
Direct Parent Indazoles
Alternative Parents Piperidinecarboxamides  Dialkylarylamines  Secondary alkylarylamines  Aminopyrimidines and derivatives  Imidolactams  Benzenoids  Pyrazoles  Heteroaromatic compounds  Secondary carboxylic acid amides  Amino acids and derivatives  Azacyclic compounds  Carbonyl compounds  Hydrocarbon derivatives  Organic oxides  Organopnictogen compounds  Primary amines  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Benzopyrazole - Indazole - 3-piperidinecarboxamide - Piperidinecarboxamide - Dialkylarylamine - Aminopyrimidine - Secondary aliphatic/aromatic amine - Imidolactam - Benzenoid - Piperidine - Pyrimidine - Azole - Heteroaromatic compound - Pyrazole - Amino acid or derivatives - Carboxamide group - Secondary carboxylic acid amide - Azacycle - Carboxylic acid derivative - Secondary amine - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Organic oxide - Amine - Carbonyl group - Organopnictogen compound - Organic oxygen compound - Organic nitrogen compound - Primary amine - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as indazoles. These are compounds containing an indazole, which is structurally characterized by a pyrazole fused to a benzene.
External Descriptors Not available

Associated Targets(Human)

AURKA Tchem Aurora kinase A (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
AURKB Tchem Aurora kinase B (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PDPK1 Tchem 3-phosphoinositide-dependent protein kinase 1 (6 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
DAPK3 Tchem Death-associated protein kinase 3 (2108 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
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHEK2 Tchem Serine/threonine-protein kinase Chk2 (4015 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDPK1 Tchem 3-phosphoinositide dependent protein kinase-1 (3758 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
CHUK Tchem Inhibitor of nuclear factor kappa B kinase alpha subunit (3170 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
ROCK1 Tclin Rho-associated protein kinase 1 (4723 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
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
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
KDR Tclin Vascular endothelial growth factor receptor 2 (20924 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ROCK2 Tclin Rho-associated protein kinase 2 (6206 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MET Tclin Hepatocyte growth factor receptor (10718 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA2 Tchem Ribosomal protein S6 kinase alpha 2 (2184 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3CG Tclin PI3-kinase p110-gamma subunit (5411 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCQ Tchem Protein kinase C theta (3319 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AKT1 Tchem Serine/threonine-protein kinase AKT (9192 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDK1 Tchem Pyruvate dehydrogenase kinase isoform 1 (2021 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SGK1 Tchem Serine/threonine-protein kinase Sgk1 (2343 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA3 Tchem Ribosomal protein S6 kinase alpha 3 (4284 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TGFBR1 Tchem TGF-beta receptor type I (3786 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP3K5 Tchem Mitogen-activated protein kinase kinase kinase 5 (1965 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
STK17A Tchem Serine/threonine-protein kinase 17A (1791 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
K562 (73714 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
U2OS (164939 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEL (6614 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HepG2 (196354 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
BRSK2 Tchem BR serine/threonine-protein kinase 2 (1562 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NLK Tchem Serine/threonine protein kinase NLK (977 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRSK1 Tchem BR serine/threonine-protein kinase 1 (2120 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NUAK1 Tchem NUAK family SNF1-like kinase 1 (1769 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKX Tchem Serine/threonine-protein kinase PRKX (2278 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SGK2 Tchem Serine/threonine-protein kinase Sgk2 (2068 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
OCI-AML2 (350 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEK-293T (167025 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

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
Fgfr3 Fibroblast growth factor receptor 3 (21 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
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

Pubchem Sid 488201269
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/488201269
IUPAC Name (3S,6R)-1-[6-(3-amino-1H-indazol-6-yl)-2-(methylamino)pyrimidin-4-yl]-N-cyclohexyl-6-methylpiperidine-3-carboxamide
INCHI InChI=1S/C25H34N8O/c1-15-8-9-17(24(34)28-18-6-4-3-5-7-18)14-33(15)22-13-20(29-25(27-2)30-22)16-10-11-19-21(12-16)31-32-23(19)26/h10-13,15,17-18H,3-9,14H2,1-2H3,(H,28,34)(H3,26,31,32)(H,27,29,30)/t15-,17+/m1/s1
InChIKey QLPHOXTXAKOFMU-WBVHZDCISA-N
Smiles CC1CCC(CN1C2=NC(=NC(=C2)C3=CC4=C(C=C3)C(=NN4)N)NC)C(=O)NC5CCCCC5
Isomeric SMILES C[C@@H]1CC[C@@H](CN1C2=NC(=NC(=C2)C3=CC4=C(C=C3)C(=NN4)N)NC)C(=O)NC5CCCCC5
WGK Germany 3
Molecular Weight 462.59
Reaxy-Rn 52299093
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=52299093&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.

22 results found

Lot Number Certificate Type Date Item
F2302391 Certificate of Analysis Apr 18, 2025 G126481
F2302853 Certificate of Analysis Apr 18, 2025 G126481
F2302393 Certificate of Analysis Apr 18, 2025 G126481
F2302388 Certificate of Analysis Apr 18, 2025 G126481
F2302390 Certificate of Analysis Apr 18, 2025 G126481
F2302397 Certificate of Analysis Apr 18, 2025 G126481
F2302849 Certificate of Analysis Mar 04, 2025 G126481
F2302395 Certificate of Analysis Mar 04, 2025 G126481
F2302387 Certificate of Analysis Mar 04, 2025 G126481
F2302396 Certificate of Analysis Mar 04, 2025 G126481
F2302389 Certificate of Analysis Mar 04, 2025 G126481
F2302392 Certificate of Analysis Mar 04, 2025 G126481
D2317175 Certificate of Analysis Feb 06, 2025 G126481
D2317164 Certificate of Analysis Feb 06, 2025 G126481
D2317176 Certificate of Analysis Feb 06, 2025 G126481
D2317174 Certificate of Analysis Feb 06, 2025 G126481
D2317177 Certificate of Analysis Feb 06, 2025 G126481
D2317178 Certificate of Analysis Feb 06, 2025 G126481
D2317185 Certificate of Analysis Feb 06, 2025 G126481
D2317179 Certificate of Analysis Feb 06, 2025 G126481
D2317166 Certificate of Analysis Feb 06, 2025 G126481
D2317158 Certificate of Analysis Mar 10, 2023 G126481

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Chemical and Physical Properties

Solubility DMSO 90 mg/mL Water <1 mg/mL Ethanol 90 mg/mL
Molecular Weight 462.600 g/mol
XLogP3 3.900
Hydrogen Bond Donor Count 4
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 5
Exact Mass 462.286 Da
Monoisotopic Mass 462.286 Da
Topological Polar Surface Area 125.000 Ų
Heavy Atom Count 34
Formal Charge 0
Complexity 688.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 2
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

Solution Calculators

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