MS-417 ( GTPL-7512 )

Catalog No. M16583 CAS No. 916489-36-6

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

MS-417
Note

Research use only, not for human use.
Brief Description

MS-417 (GTPL-7512) is a highly specific BET bromodomain inhibitor that binds to BRD4-BD1 and BRD4 BD2 with Kd of 36.1 uM and 25.4 uM respectively.
Description

MS-417 (GTPL-7512) is a highly specific BET bromodomain inhibitor that binds to BRD4-BD1 and BRD4 BD2 with Kd of 36.1 uM and 25.4 uM respectively; shows 100-200-fold weaker affinity for CBP, BRD7, or BPTF, and no binding affinity for many other bromodomains; blocks BRD4 binding to the acetylated NF-κB, effectively attenuates NF-κB transcriptional activation of proinflammatory genes in kidney cells treated with TNFα or infected by HIV; ameliorates inflammation and kidney injury in HIV-1 transgenic mice.
Synonyms

GTPL-7512
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

——
Indication

——

CAS Number

916489-36-6
Formula Weight

414.91
Molecular Formula

C20H19ClN4O2S
Purity

>98% (HPLC)
Solubility

Ethanol : 50 mg/mL 120.51 mM
SMILES

CC1=C(SC2=C1C(=N[C@H](C3=NN=C(N32)C)CC(=O)OC)C4=CC=C(C=C4)Cl)C
Chemical Name

Methyl 2-[(6S,Z)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetate

1. Zhang G, et al. J Biol Chem. 2012 Aug 17;287(34):28840-51.
2. Boehm D, et al. Cell Cycle. 2013 Feb 1;12(3):452-62.

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