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Chemical Structure| 916489-36-6 Chemical Structure| 916489-36-6

Structure of MS417
CAS No.: 916489-36-6

Chemical Structure| 916489-36-6

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MS417 is a selective BET protein BRD4 inhibitor that binds to BRD4-BD1 and BRD4-BD2, suitable for research in epigenetics and oncology.

Synonyms: GTPL7512

4.5 *For Research Use Only! Not for Human Use. We Do Not Sell to Patients.

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Product Details of MS417

CAS No. :916489-36-6
Formula : C20H19ClN4O2S
M.W : 414.91
SMILES Code : CC1=C(C)SC2=C1C(C3=CC=C(Cl)C=C3)=N[C@@H](CC(OC)=O)C4=NN=C(C)N24
Synonyms :
GTPL7512
English Name :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
MDL No. :MFCD20526583

Safety of MS417

Related Pathways of MS417

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
SW620 1 µM 48 h To evaluate the effect of MS417 on SW620 cell migration and invasion, results showed that MS417 significantly inhibited SW620 cell migration and invasion. Int J Mol Sci. 2015 Jan 16;16(1):1928-48
HT29 1 µM 48 h To evaluate the effect of MS417 on HT29 cell migration and invasion, results showed that MS417 significantly inhibited HT29 cell migration and invasion. Int J Mol Sci. 2015 Jan 16;16(1):1928-48
SW620 1 µM 10 days To evaluate the effect of MS417 on SW620 colony formation, results showed that MS417 significantly reduced the number and size of SW620 colonies. Int J Mol Sci. 2015 Jan 16;16(1):1928-48
HT29 1 µM 10 days To evaluate the effect of MS417 on HT29 colony formation, results showed that MS417 significantly reduced the number and size of HT29 colonies. Int J Mol Sci. 2015 Jan 16;16(1):1928-48
SW620 1, 3, 6, 9, 12, 24, 30 µM 24, 48, 72 h To evaluate the effect of MS417 on SW620 cell proliferation, results showed that MS417 significantly inhibited SW620 cell proliferation, but with lower sensitivity compared to HT29 cells. Int J Mol Sci. 2015 Jan 16;16(1):1928-48
HT29 1, 3, 6, 9, 12, 24, 30 µM 24, 48, 72 h To evaluate the effect of MS417 on HT29 cell proliferation, results showed that MS417 significantly inhibited HT29 cell proliferation in a dose- and time-dependent manner. Int J Mol Sci. 2015 Jan 16;16(1):1928-48
neonatal rat cardiomyocytes (NRCMs) 1μM 6 hours Inhibited ISO-induced hypertrophic responses in cardiomyocytes Acta Pharm Sin B. 2021 May;11(5):1286-1299
Primary mouse hepatocytes 50 nM 24 hours To assess the role of BRD4 in hepatocellular lipotoxicity, MS417 reduced PA-induced lipid droplet accumulation Cell Mol Life Sci. 2024 Jul 9;81(1):295
AML12 hepatocytes 50 nM 24 hours To evaluate the effect of BRD4 on lipid droplet accumulation in hepatocellular lipotoxicity, MS417 significantly reduced PA-induced lipid droplet deposition Cell Mol Life Sci. 2024 Jul 9;81(1):295
human podocytes 1.0 μmol/L 24 hours MS417 inhibited AGE-induced acetylation and phosphorylation of p65 and STAT3 Diabetes. 2014 Jul;63(7):2440-53
293T cells 1.0 µM 24 hours To assess the inhibitory effect of MS417 on TNFα-induced NF-κB transcriptional activity. Results showed that MS417 nearly completely suppressed NF-κB activation at 1.0 µM concentration. J Biol Chem. 2012 Aug 17;287(34):28840-51
human renal tubular epithelial cells (RTECs) 1.0 µM 24 hours To evaluate the inhibitory effect of MS417 on NF-κB transcriptional activity in HIV-infected RTECs. Results showed that MS417 significantly suppressed HIV-induced transcriptional activation of NF-κB target genes (e.g., CCL2, CCL20). J Biol Chem. 2012 Aug 17;287(34):28840-51

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c-nu nude mice HT29 and SW620 xenograft model Intraperitoneal injection 20 mg/kg Every 2 days for 3 weeks To evaluate the effect of MS417 on HT29 and SW620 xenograft tumor growth, results showed that MS417 significantly inhibited tumor growth and volume. Int J Mol Sci. 2015 Jan 16;16(1):1928-48
HIV-1 transgenic mice (Tg26) HIV-associated nephropathy model Oral gavage 0.08 mg/kg Once daily for 4 weeks To evaluate the therapeutic effect of MS417 on HIV-associated nephropathy. Results showed that MS417 significantly improved renal function, reduced proteinuria, and attenuated kidney inflammation and injury in Tg26 mice. J Biol Chem. 2012 Aug 17;287(34):28840-51
Mice Diabetic db/db mice Gavage 0.08 mg/kg Daily for 12 weeks MS417 significantly reduced proteinuria and mesangial expansion Diabetes. 2014 Jul;63(7):2440-53

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.05mL

2.41mL

1.21mL

24.10mL

4.82mL

2.41mL

 

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