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BI-2536

Inh 755038-02-9 4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide

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Catalog No. ABIN7233234

Datasheet as PDF

Application

Inhibition (Inh)

Purpose

Dual Plk/BRD4 inhibitor, Destabilizes Myc

Characteristics

BI 2536 was originally reported as a potent (IC50's Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM) and selective2 Polo-like kinase inhibitor (IC50's Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM) that caused mitotic arrest and apoptosis induction in various human cancer cell lines. It was later found to be a potent inhibitor (IC50 = 100nM) of BET family member BRD4 and able to potently suppress c-Myc expression in MM.1S multiple myeloma cells. BI 2536 destabilizes N-Myc by inhibiting the deactivation of the ubiquitin E3 ligase Fbw7 by Plk1.

Purity

>97 %

Chemical Name

4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide

Formula

C28H39N7O3

Solubility

Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 25 mg/ml)
Geldanamycin
Inh 30562-34-6 (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1] docosa-1(21),4,6,10,18-pentaen-9-yl carbamate

Radicicol
Inh 12772-57-5

Geldanamycin- FITC
Inh 30562-34-6 (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1] docosa-1(21),4,6,10,18-pentaen-9-yl carbamate

Nicotinamide
Inh 98-92-0 Pyridine-3-carboxylic acid amide

5-Azacytidine
Inh Cell-permeable 320-67-2 4-Amino-1-ß-D-ribofuranosyl-1,3,5-triazin-2(1H)-one

SAHA (Vorinostat)
Inh Cell-permeable 149647-78-9 Suberoylanilide-hydroxamic acid

Phenylbutyrate Na
Inh 1716-12-7 4-Phenylbutyric acid, sodium salt

CI-994
Inh 112522-64-2 4-(Acetylamino)-N-(2-aminophenyl)benzamide

Tranylcypromine hemisulfate (±)
Inh Cell-permeable 13492-01-8 Trans (±)-2-phenylcyclopropanamine, hemisulfate salt

Tenovin-1
Inh 380315-80-0 N-[(4-Acetamidophenyl)carbamothioyl]-4-tert-butylbenzamide

Restrictions

For Research Use only
Format

Powder

Storage

-20 °C
Background

Apoptosis inducer,Epigenetics,Cell cycle,Myc,Bromodomain,Ubiquitin/Proteasome,Cell death,Cancer,Posttranslational modification,Chromatin

Molecular Weight

521.67

CAS-No

755038-02-9