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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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产品编号 ABIN7233234

发货至: 中国

Datasheet as PDF

应用范围

Inhibition (Inh)

原理

Dual Plk/BRD4 inhibitor, Destabilizes Myc

产品特性

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.

纯度

>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

Resveratrol
Act 501-36-0 3,4',5-Trihydroxy-trans-stilbene

Panobinostat
Inh 404950-80-7 (E)-N-Hydroxy-3-(4-((2-(2-methyl-1H-indol-3-yl)ethylamino)methyl)phenyl)acrylamide

HPA (Hexyl-4-pentynoic acid)
Inh Cell-permeable 96017-59-3 2-(2-Propynyl)octanoic acid (racemic)

EX-527
Inh Cell-permeable 49843-98-3 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-xarboxamide (racemic)

Daminozide
Inh 1596-84-5 1-(2,2-Dimethylhydrazide)butanedioic acid

Mithramycin A
Inh 18378-89-7

Piceatannol
Inh 10083-24-6 3,3',4,5'-Tetrahydroxy-trans-stilbene

限制

仅限研究用
状态

Powder

储存条件

-20 °C
背景

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

分子量

521.67

CAS-编号

755038-02-9