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MS417 (also known as GTPL7512) is a potent and selective BRD4 inhibitor, which binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30 and 46 nM, respectively. MS417 effectively blocks BRD4 binding to NF-κB, almost completely suppresses TNFα-induced NF-κB transcription activation in human embryonic kidney 293T cells at 1 μM and also reduces NF-κB p65 acetylation in the HIV-infected RTECs. MS417 (1 μM) modulation of gene transcription in HIV-infected human primary renal tubular epithelial cells.
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.
| Molecular Weight | 414.91 |
| Formula | C20H19ClN4O2S |
| CAS Number | 916489-36-6 |
| Solubility (25°C) | Ethanol ≥ 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Epigenetic Reader Domain Products |
|---|
| dBRD9 dihydrochloride
dBRD9 dihydrochloride is a selective BRD9 PROTAC degrader. |
| BBC0403
BBC0403 is a selective BRD2 inhibitor with Kds of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. |
| BAY-155
BAY-155 is a potent and selective menin-MLL tool inhibitor, with an IC50 of 8 nM. |
| FHT-1015
FHT-1015 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM. |
| ISOX-DUAL
ISOX-DUAL is a dual CBP/BRD4 inhibitor with IC50 values of 0.65 μM and 1.5 μM for CBP and BRD4, respectively. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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