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
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
N-Bromosuccinimide Price
- Product number
- SML2442
- Product name
- MS417
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $126.35
- Updated
- 2025/07/31
- Product number
- SML2442
- Product name
- MS417
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $346
- Updated
- 2025/07/31
- Product number
- CS-0034388
- Product name
- MS417
- Purity
- 99.51%
- Packaging
- 5mg
- Price
- $100
- Updated
- 2021/12/16
- Product number
- CS-0034388
- Product name
- MS417
- Purity
- 99.51%
- Packaging
- 10mg
- Price
- $160
- Updated
- 2021/12/16
- Product number
- CS-0034388
- Product name
- MS417
- Purity
- 99.51%
- Packaging
- 50mg
- Price
- $420
- Updated
- 2021/12/16
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
MS417 Suppliers
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- +1-781-999-5354; +17819995354
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- Country
- United States
- ProdList
- 32435
- Advantage
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- tp@aladdinsci.com
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