Free shipping on all orders over $ 500

MS417

Cat. No. M9515
MS417 Structure
Synonym:

GTPL7512

Size Price Availability Quantity
5mg USD 90  USD90 In stock
10mg USD 140  USD140 In stock
50mg USD 370  USD370 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Zhang G, et al. J Biol Chem. Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition.

Related Epigenetic Reader Domain Products
Phoenixin-20

Phoenixin-20 (PNX-20) is a bioactive peptide with hormone-like actions in vertebrates, and can stimulates hypothalamo-pituitary-gonadal hormones and regulate reproductive processes in mammals.

Menin-MLL inhibitor 31

Menin-MLL inhibitor 31 is a potent inhibitor of the menin MLL interaction with an IC50 value of 4.6 nM.

OPN-2853

OPN-2853 is a bromodomain protein-4 (BRD4) inhibitor that can be used in studies related to hematologic and lymphatic disorders.

HDAC/JAK/BRD4-IN-1

HDAC/JAK/BRD4-IN-1 is a potent HDAC/JAK/BRD4 triple inhibitor.

VYN-201

VYN-201 is a novel pan-BET inhibitor for studies related to idiopathic pulmonary fibrosis.

  Catalog
Abmole Inhibitor Catalog




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


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.