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MS417

Cat. No. M9515
MS417 Structure
Synonym:

GTPL7512

Size Price Availability Quantity
5mg USD 247 In stock
10mg USD 345 In stock
25mg USD 687 In stock
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 414.91
Formula C20H19ClN4O2S
CAS Number 916489-36-6
Purity >98.5%
Solubility Ethanol ≥ 10 mg/mL
Storage at -20°C
References

Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition.
Zhang G, et al. J Biol Chem. 2012 Aug 17;287(34):28840-51. PMID: 22645123.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MS417, GTPL7512 supplier, Epigenetic Reader Domain, inhibitors

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