biBET( BiBET )

Catalog No. M13200 CAS No. 2059110-46-0

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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Product Name

biBET
Note

Research use only, not for human use.
Brief Description

biBET is a potent, selective, bivalent inhibitor of BET bromodomains.
Description

biBET is a potent, selective, bivalent inhibitor of BET bromodomains with pKd of 8.3/7.3/11 for BRD4(1)/BRD4(2)/BRD4(1,2), respectively; exhibts very high cellular potency for BRD4 binding and pharmacological responses such as disruption of BRD4-mediator complex subunit 1 foci with an EC50 of 100 pM; an useful BET/BRD4 chemical probe.
In Vitro

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In Vivo

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Synonyms

BiBET
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

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Indication

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CAS Number

2059110-46-0
Formula Weight

530.593
Molecular Formula

C26H30N10O3
Purity

>98% (HPLC)
Solubility

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SMILES

CN(CCOC1=CC=C(C2CCN(C3=NN4C(C=C3)=NN=C4OC)CC2)C=C1)C5=NN6C(C=C5)=NN=C6OC
Chemical Name

3-Methoxy-N-(2-(4-(1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)-N-methyl-[1,2,4]triazolo[4,3-b]pyridazin-6-amine

1. Waring MJ, et al. Nat Chem Biol. 2016 Dec;12(12):1097-1104.

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