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OSU-03012 (AR-12) - ≥98%, high purity , 3-phosphoinositide dependent protein kinase-1 inhibitor, CAS No.742112-33-0, 3-phosphoinositide dependent protein kinase-1 inhibitor

COA COA
In stock
Item Number
O126958
Grouped product items
SKU Size
Availability
 Price Qty
O126958-5mg
5mg
3
$127.90
O126958-25mg
25mg
3
$443.90
O126958-100mg
100mg
2
$1,270.90
Wish List
Bulk Order  SDS  DATASHEET  Specification Sheet

PDPK1 (PDK1) inhibitor; inhibits Akt signaling

View related series
3-phosphoinositide dependent protein kinase 1 Inhibitor (7) Autophagy (1917)

Basic Description

Synonyms PDK1 inhibitor AR-12 | 9-Fluoro-11beta,17,21-trihydroxypregna-1,4-diene-3,20-dione 21-acetate | DTXSID50225206 | AS-19550 | OSU-03012 | FT-0721533 | N-(4-(5-(2-Phenanthryl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)ethane-1,2-diamine | SCHEMBL570472 | AR
Specifications & Purity Moligand™, ≥98%
Biochemical and Physiological Mechanisms PDPK1 (PDK1) inhibitor; inhibits Akt signaling. Induces apoptosis of PC-3 and medulloblastoma cells, and inhibits growth of a number of tumor cell lines. Sensitizes radiotherapy-induced cell death and enhances cytotoxic effects of chemotherapeutic agentsi
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 3-phosphoinositide dependent protein kinase-1 inhibitor
Product Description

OSU-03012 is a potent inhibitor of recombinant PDK-1 with IC50 of 5 μM and 2-fold increase in potency over OSU-02067.
A PDK1 inhibitor and inducer of caspase and p53-independent apoptosis.

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Benzenoids
Class Phenanthrenes and derivatives
Subclass Not available
Intermediate Tree Nodes Not available
Direct Parent Phenanthrenes and derivatives
Alternative Parents Alpha amino acid amides  Phenylpyrazoles  Naphthalenes  Anilides  N-arylamides  Heteroaromatic compounds  Secondary carboxylic acid amides  Azacyclic compounds  Organopnictogen compounds  Organofluorides  Organic oxides  Monoalkylamines  Hydrocarbon derivatives  Carbonyl compounds  Alkyl fluorides  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Phenanthrene - Alpha-amino acid amide - Phenylpyrazole - Alpha-amino acid or derivatives - Naphthalene - Anilide - N-arylamide - Monocyclic benzene moiety - Azole - Heteroaromatic compound - Pyrazole - Amino acid or derivatives - Carboxamide group - Secondary carboxylic acid amide - Azacycle - Carboxylic acid derivative - Organoheterocyclic compound - Organofluoride - Organohalogen compound - Organic nitrogen compound - Primary aliphatic amine - Alkyl halide - Alkyl fluoride - Carbonyl group - Hydrocarbon derivative - Organic oxide - Organopnictogen compound - Amine - Organic oxygen compound - Organonitrogen compound - Organooxygen compound - Primary amine - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene.
External Descriptors Not available

Product Properties

ALogP 5.2

Associated Targets(Human)

PDPK1 Tchem 3-phosphoinositide-dependent protein kinase 1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
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
A673 (619 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CAKI-1 (44928 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HT-29 (80576 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Huh-7 (12904 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MCF7 (126967 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PC-3 (62116 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SK-N-MC (815 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
786-0 (47912 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NCI-H69 (709 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HCT-116 (91556 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEK293 (82097 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
IGROV-1 (47897 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NCI-H82 (178 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TC-32 (111 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
Pseudomonas aeruginosa (123386 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Klebsiella pneumoniae (43867 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Salmonella typhimurium (15756 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Staphylococcus aureus (210822 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Staphylococcus epidermidis (22802 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Acinetobacter baumannii (41033 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Escherichia coli (133304 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cryptococcus neoformans (21258 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Candida albicans (78123 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
dengue virus type 4 (242 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RAW264.7 (28094 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
Akt1 RAC-alpha serine/threonine-protein kinase (147 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
dengue virus type 1 (258 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
dengue virus type 2 (2400 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
dengue virus type 3 (207 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Lassa virus (234 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Nipah virus (19 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Marburgvirus (118 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Zika virus (1028 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Ebolavirus (617 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 2-amino-N-[4-[5-phenanthren-2-yl-3-(trifluoromethyl)pyrazol-1-yl]phenyl]acetamide
INCHI InChI=1S/C26H19F3N4O/c27-26(28,29)24-14-23(33(32-24)20-10-8-19(9-11-20)31-25(34)15-30)18-7-12-22-17(13-18)6-5-16-3-1-2-4-21(16)22/h1-14H,15,30H2,(H,31,34)
InChIKey YULUCECVQOCQFQ-UHFFFAOYSA-N
Smiles C1=CC=C2C(=C1)C=CC3=C2C=CC(=C3)C4=CC(=NN4C5=CC=C(C=C5)NC(=O)CN)C(F)(F)F
Isomeric SMILES C1=CC=C2C(=C1)C=CC3=C2C=CC(=C3)C4=CC(=NN4C5=CC=C(C=C5)NC(=O)CN)C(F)(F)F
Molecular Weight 460.46
Reaxy-Rn 11001693
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11001693&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.

1 results found

Lot Number Certificate Type Date Item
G1521072 Certificate of Analysis Nov 13, 2024 O126958

Chemical and Physical Properties

Solubility Solvent:DMSO, Max Conc. mg/mL: 46.05, Max Conc. mM: 100
Melt Point(°C) 177-180°C
Molecular Weight 460.400 g/mol
XLogP3 5.200
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 6
Rotatable Bond Count 4
Exact Mass 460.151 Da
Monoisotopic Mass 460.151 Da
Topological Polar Surface Area 72.900 Ų
Heavy Atom Count 34
Formal Charge 0
Complexity 711.000
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

Solution Calculators

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