L-45 ( PCAF BRD inhibitor L-45 )

Catalog No. M13235 CAS No. 2079885-05-3

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Datasheet

HNMR

HPLC

MSDS

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Product Name

L-45
Note

Research use only, not for human use.
Brief Description

PCAF BRD inhibitor L-45 is a potent, selective, and cell-active PCAF bromodomain inhibitor with Ki of 47 nM in HTRF assays.
Description

PCAF BRD inhibitor L-45 is a potent, selective, and cell-active PCAF bromodomain inhibitor with Ki of 47 nM in HTRF assays, >4,500-fold selectivity over BRD4; disrupt PCAF-Brd histone H3.3 interaction in cells using a nanoBRET assay, shows high selectivity for PCAF and GCN5 bromodomain (Kd=600 nM); shows no observable cytotoxicity in PBMCs, good cell-permeability, and metabolic stability in human and mouse liver microsomes.
Synonyms

PCAF BRD inhibitor L-45
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

Cancer
Indication

——

CAS Number

2079885-05-3
Formula Weight

360.47
Molecular Formula

C21H24N6
Purity

>98% (HPLC)
Solubility

——
SMILES

C[C@H](NC(C1=C2C=CC=C1)=NN3C2=NN=C3C)[C@H](C4=CC=CC=C4)N(C)C
Chemical Name

(1S,2S)-N1,N1-dimethyl-N2-(3-methyl-[1,2,4]triazolo[3,4-a]phthalazin-6-yl)-1-phenylpropane-1,2-diamine

1. Moustakim M, et al. Angew Chem Int Ed Engl. 2017 Jan 16;56(3):827-831.

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