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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

Moligand™
≥98%

CAS#: 742112-33-0
Formula: C₂₆H₁₉F₃N₄O
Molecular Weight: 460.46
PubChem CID: 10027278

Item Number

O126958

Grouped product items
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

PDPK1 (PDK1) inhibitor; inhibits Akt signaling

View related series

3-phosphoinositide dependent protein kinase 1 Inhibitor

Basic Description

Synonyms	OSU-03012\|742112-33-0\|AR-12\|PDK1 inhibitor AR-12\|OSU 03012\|OSU-03012 (AR-12)\|2-amino-N-(4-(5-(phenanthren-2-yl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)acetamide\|OSU03012\|2-amino-N-[4-[5-phenanthren-2-yl-3-(trifluoromethyl)pyrazol-1-yl]phenyl]acetamide
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.

Associated Targets

HDAC6 Tclin Histone deacetylase 6 0 Activities

Discover Target: HDAC6

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

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 0 Activities

Discover Target: AKT1

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

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)

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

PubChem CID

ChEMBL Ligand

CAS Registry No.

Wikipedia

RCSB PDB Ligand

Certificates

Certificate of Analysis(COA)

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1 results found

Lot Number	Certificate Type	Date	Item
G1521072	Certificate of Analysis	Feb 03, 2023	O126958

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]
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]
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]

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