Grouped product items

SKU

Size

Availability

Price

Qty

O126958-5mg

5mg

Available within 4-8 weeks(?)

$127.90

O126958-25mg

25mg

Available within 4-8 weeks(?)

$443.90

O126958-100mg

100mg

Available within 4-8 weeks(?)

$1,270.90

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
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	3-phosphoinositide dependent protein kinase-1 inhibitor
Note	卖完停产，不再备货
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.

Product Properties

ALogP	5.2

Associated Targets(Human)

PDPK1 Tchem 3-phosphoinositide-dependent protein kinase 1 (1 Activities)

Discover Target: PDPK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDPK1 Tchem 3-phosphoinositide dependent protein kinase-1 (3758 Activities)

Discover Target: PDPK1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

A673 (619 Activities)

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CAKI-1 (44928 Activities)

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HT-29 (80576 Activities)

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Huh-7 (12904 Activities)

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MCF7 (126967 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PC-3 (62116 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SK-N-MC (815 Activities)

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786-0 (47912 Activities)

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NCI-H69 (709 Activities)

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HCT-116 (91556 Activities)

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HEK293 (82097 Activities)

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HepG2 (196354 Activities)

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IGROV-1 (47897 Activities)

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NCI-H82 (178 Activities)

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TC-32 (111 Activities)

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Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)

Discover Target: Hdac6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Pseudomonas aeruginosa (123386 Activities)

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Klebsiella pneumoniae (43867 Activities)

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Salmonella typhimurium (15756 Activities)

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Staphylococcus aureus (210822 Activities)

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Staphylococcus epidermidis (22802 Activities)

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Acinetobacter baumannii (41033 Activities)

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Escherichia coli (133304 Activities)

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Cryptococcus neoformans (21258 Activities)

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Candida albicans (78123 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

dengue virus type 4 (242 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

RAW264.7 (28094 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

rep Replicase polyprotein 1ab (378 Activities)

Discover Target: rep

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Akt1 RAC-alpha serine/threonine-protein kinase (147 Activities)

Discover Target: Akt1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

dengue virus type 1 (258 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

dengue virus type 2 (2400 Activities)

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dengue virus type 3 (207 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Lassa virus (234 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Nipah virus (19 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Marburgvirus (118 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Zika virus (1028 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SARS-CoV-2 (38078 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Ebolavirus (617 Activities)

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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)
InChi Key	YULUCECVQOCQFQ-UHFFFAOYSA-N
Canonical 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
PubChem CID	10027278
Molecular Weight	460.46

Database links

PubChem CID	10027278
ChEMBL Ligand	CHEMBL1650595
CAS Registry No.	742112-33-0
Wikipedia	OSU-03012
RCSB PDB Ligand	M4J

Certificates

Certificate of Analysis(COA)

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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

References

1. Shiojima I, Walsh K. (2002) Role of Akt signaling in vascular homeostasis and angiogenesis.. Circ Res, 90 (12): (1243-50). [PMID:12089061] [10.1021/op500134e]
2. Hanada M, Feng J, Hemmings BA. (2004) Structure, regulation and function of PKB/AKT--a major therapeutic target.. Biochim Biophys Acta, 1697 (1-2): (3-16). [PMID:15023346] [10.1021/op500134e]
3. Zhu J, Huang JW, Tseng PH, Yang YT, Fowble J, Shiau CW, Shaw YJ, Kulp SK, Chen CS. (2004) From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors.. Cancer Res, 64 (12): (4309-18). [PMID:15205346] [10.1021/op500134e]

Solution Calculators

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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

Basic Description

Product Properties

Associated Targets(Human)

Associated Targets(non-human)

Mechanisms of Action

Names and Identifiers

Database links

Certificates

Certificate of Analysis(COA)

Chemical and Physical Properties

Related Documents

References

Solution Calculators

Molarity Calculator

Dilution Calculator

Reconstitution Calculator

SKU	Size	Availability	Price
O126958-5mg	5mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$127.90
O126958-25mg	25mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$443.90
O126958-100mg	100mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$1,270.90