Favorite  |  Set Home
Products > Others > > MS436
Product name : MS436
Item : CR1872
Price : 100mg, $945; 200mg, $1485
contact : Send inquiry to: info@acesobio.com
Additional Information :  We offer significant discount for bulky quantity order,Please ask price and availability of other quantities
CAS : 395084-25-9
 Enlarge Image                   Back
←[Previous Product]              [Next Product]→


Details:
 Chemical Information
M.Wt 383.42 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C18H17N5O3S
CAS No 1395084-25-9
Solubility

DMSO



Biological Activity of MS436

 

MS436 is a diazobenzene-based small-molecule inhibitor for the BRD4 bromodomains with a Ki value of 30-50 nM.
IC50 Value: 30-50 nM (Ki) [1]
Target: BRD4 bromodomain
MS436 exhibits low nanomolar affinity (estimated Ki of 30-50 nM), with preference for the first bromodomain over the second. MS436 effectively inhibits BRD4 activity in NF-κB-directed production of nitric oxide and proinflammatory cytokine interleukin-6 in murine macrophages. MS436 represents a new class of bromodomain inhibitors and will facilitate further investigation of the biological functions of the two bromodomains of BRD4 in gene expression [1] .
 

 

[1]. Zhang G, et al. Structure-Guided Design of Potent Diazobenzene Inhibitors for the BET Bromodomains. J Med Chem. 2013 Nov 27;56(22):9251-64.
Abstract
BRD4, characterized by two acetyl-lysine binding bromodomains and an extra-terminal (ET) domain, is a key chromatin organizer that directs gene activation in chromatin through transcription factor recruitment, enhancer assembly, and pause release of the RNA polymerase II complex for transcription elongation. BRD4 has been recently validated as a new epigenetic drug target for cancer and inflammation. Our current knowledge of the functional differences of the two bromodomains of BRD4, however, is limited and is hindered by the lack of selective inhibitors. Here, we report our structure-guided development of diazobenzene-based small-molecule inhibitors for the BRD4 bromodomains that have over 90% sequence identity at the acetyl-lysine binding site. Our lead compound, MS436, through a set of water-mediated interactions, exhibits low nanomolar affinity (estimated Ki of 30-50 nM), with preference for the first bromodomain over the second. We demonstrated that MS436 effectively inhibits BRD4 activity in NF-κB-directed production of nitric oxide and proinflammatory cytokine interleukin-6 in murine macrophages. MS436 represents a new class of bromodomain inhibitors and will facilitate further investigation of the biological functions of the two bromodomains of BRD4 in gene expression.


Related Products :
URB 754
URB 754
Price: 10mg, $45; 50mg, $145; 100mg, $225; 200mg, $455
HQL 79
HQL 79
Price: 10mg, $125; 50mg, $495; 100mg, $895; 200mg, $1495
LDN 192960
LDN 192960
Price: 10mg, $295; 50mg, $895; 100mg, $1495; 200mg, $2195
SR 48692
SR 48692
Price: 10mg, $195; 50mg, $675; 100mg, $965; 200mg, $1655
OC 000459
OC 000459
Price: 10mg, $195; 50mg, $795; 100mg,$1295; 200mg, $2155
WZ 811
WZ 811
Price: 10mg, $125; 50mg, $495; 100mg, $695; 200mg, $995
Ezetimib
Ezetimib
Price: 10mg, $25; 50mg, $75; 100mg, $95; 200mg, $175
Duloxetine
Duloxetine
Price: 10mg, $125; 50mg, $495; 100mg, $695; 200mg, $1095