Poloxin

Poloxin is the first small-molecule inhibitor specifically targeting the function of the Plk1 PBD. Poloxin induces centrosome fragmentation and abnormal spindle and chromosome misalignment, which activate the spindle assembly checkpoint and prolong mitosis. Notably, centrosomal fragmentation induced by Poloxin is partially attributable to dysfunctional Kizuna, a key substrate of Plk1 at centrosomes. Moreover, Poloxin strongly inhibits proliferation of a panel of cancer cells by inducing mitotic arrest, followed by a surge of apoptosis. More important, we report, for the first time to our knowledge, that the PBD inhibitor, Poloxin , significantly suppresses tumor growth of cancer cell lines in xenograft mouse models by lowering the proliferation rate and triggering apoptosis in treated tumor tissues. Targeting the PBD by Poloxin is a powerful approach for selectively inhibiting Plk1 function in vitro and in vivo. ( Am J Pathol. 2011 Oct;179(4):2091-9. ). (2/18/2014)

Product information

CAS Number: 321688-88-4

Molecular Weight: 297.35

Formula: C18H19NO3

Chemical Name: [(1Z)-2-methyl-4-oxo-5-(propan-2-yl)cyclohexa-2,5-dien-1-ylidene]amino 2-methylbenzoate

Smiles: CC1=CC=CC=C1C(=O)O/N=C1/C=C(C(C)C)C(=O)C=C/1C

InChiKey: CMOJHDQJJPIVEC-MNDPQUGUSA-N

InChi: InChI=1S/C18H19NO3/c1-11(2)15-10-16(13(4)9-17(15)20)19-22-18(21)14-8-6-5-7-12(14)3/h5-11H,1-4H3/b19-16-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.