SKP2-C25 --- Skp2 Inhibitor

SKP2-C25 is a potent, selective and cell permeable Skp2 inhibitor. It selectively inhibits Skp2 E3 ligase activity, but not activity of other SCF complexes. It also phenocopies the effects observed upon genetic Skp2 deficiency, such as suppressing survival and Akt-mediated glycolysis and triggering p53-independent cellular senescence. SKP2-C25 exhibits potent antitumor activities in multiple animal models and cooperates with chemotherapeutic agents to reduce cancer cell survival. It is a useful chemical probe to target Skp2, which is a promising target for restricting cancer stem cell and cancer progression.

Product information

CAS Number: 222716-34-9

Molecular Weight: 420.52

Formula: C24H24N2O3S

Synonym:

SZL P1-41

Chemical Name: 3-(benzo[d]thiazol-2-yl)-6-ethyl-7-hydroxy-8-(piperidin-1-ylmethyl)-4H-chromen-4-one

Smiles: CCC1=CC2C(=O)C(=COC=2C(CN2CCCCC2)=C1O)C1=NC2=CC=CC=C2S1

InChiKey: JKIXLEKBXHMXTN-UHFFFAOYSA-N

InChi: InChI=1S/C24H24N2O3S/c1-2-15-12-16-22(28)18(24-25-19-8-4-5-9-20(19)30-24)14-29-23(16)17(21(15)27)13-26-10-6-3-7-11-26/h4-5,8-9,12,14,27H,2-3,6-7,10-11,13H2,1H3

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO up to 50 mM

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: ≥12 months 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

How to use

In Vitro:

SKP2-C25 was used at 5-20 µM final concentration in various in vitro assays.

In Vivo:

SKP2-C25 was administered once per day by IP injection at 40-80 mg/kg in mice with A549 or PC3 tumor xenografts for 3-5 weeks.

References:

1. Chan CH, et al. Pharmacological Inactivation of Skp2 SCF Ubiquitin Ligase Restricts Cancer Stem Cell Traits and Cancer Progression. (2013) Cell. 154(3):556-68.

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

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