ChemicalBook > CAS DataBase List > MS417

MS417

Product Name
MS417
CAS No.
916489-36-6
Chemical Name
MS417
Synonyms
MS147;MS417;GTPL7512;MS-417; M S417;MS417(GTPL7512);methyl(S)-2-(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;(S)-methyl 2-(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;Epigenetic Reader Domain,inhibit,MS417,HIV,MS 417,GTPL 7512,Inhibitor,MS-417,GTPL-7512,Human immunodeficiency virus;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;6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid, 4-(4-chlorophenyl)-2,3,9-trimethyl-, methyl ester, (6S)-
CBNumber
CB92748943
Molecular Formula
C20H19ClN4O2S
Formula Weight
414.91
MOL File
916489-36-6.mol
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MS417 Property

Boiling point:
596.8±60.0 °C(Predicted)
Density 
1.43±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
Ethanol : 50 mg/mL (120.51 mM)
form 
Solid
pka
1.86±0.60(Predicted)
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2442
Product name
MS417
Purity
≥98% (HPLC)
Packaging
5mg
Price
$126.35
Updated
2025/07/31
Sigma-Aldrich
Product number
SML2442
Product name
MS417
Purity
≥98% (HPLC)
Packaging
25mg
Price
$346
Updated
2025/07/31
ChemScene
Product number
CS-0034388
Product name
MS417
Purity
99.51%
Packaging
50mg
Price
$420
Updated
2021/12/16
ChemScene
Product number
CS-0034388
Product name
MS417
Purity
99.51%
Packaging
100mg
Price
$700
Updated
2021/12/16
ChemScene
Product number
CS-0034388
Product name
MS417
Purity
99.51%
Packaging
250mg
Price
$1300
Updated
2021/12/16
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MS417 Chemical Properties,Usage,Production

Uses

MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM).

Definition

ChEBI: MS-417 is a member of the class of thienotriazolodiazepines that is the methyl ester of [(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetic acid. A bromodomain and extra-terminal domain (BET)-specific inhibitor that belongs to a group of thienodiazepine-based compounds It is a thienotriazolodiazepine, a member of monochlorobenzenes and a methyl ester. It is an enantiomer of a MS-566.

Biological Activity

MS417, a (+)-JQ1 analog, is a potent inhibitor of bromodomain-containing protein 4 (BRD4) th at is highly specific for BRD4-BD1 and BRD4-BD2. MS417 binds with similar affinity to BRD4-BD1 and BRD4-BD2 (Kd =36.1, and 25.4 nM), while bulky tBu of JQ1 prevents tight binding to the cavity at BD1.

in vivo

MS417 (0.08 mg/kg) markedly improves renal function, reduces proteinuria and decreases glomerulosclerosis, tubular injury, and infiltration of inflammatory cells in the kidney of Tg26 mice[1].

References

[1] Zhang G, et al. Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition. J Biol Chem. 2012 Aug 17;287(34):28840-51. DOI:10.1074/jbc.M112.359505

MS417 Preparation Products And Raw materials

Raw materials

Preparation Products

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916489-36-6, MS417Related Search:


  • MS417
  • (S)-methyl 2-(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
  • MS-417; M S417
  • GTPL7512
  • 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid, 4-(4-chlorophenyl)-2,3,9-trimethyl-, methyl ester, (6S)-
  • Epigenetic Reader Domain,inhibit,MS417,HIV,MS 417,GTPL 7512,Inhibitor,MS-417,GTPL-7512,Human immunodeficiency virus
  • methyl(S)-2-(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
  • MS147
  • 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
  • methyl 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetraazatricyclo[8.3.0.02,?]trideca-2(6),4,7,10,12-pentaen-9-yl]acetate
  • MS417(GTPL7512)
  • 916489-36-6