PFI-1

CHF 60.00
In stock
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Product Details
Synonyms 2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide; PF-06405761
Product Type Chemical
Properties
Formula C16H17N3O4S
MW 347.4
CAS 1403764-72-6
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO.
Declaration Manufactured by SynKinase.
Other Product Data Target: BET, BrD4 | Kinase Group: N/A | Substrate: N/A

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
InChi Key TXZPMHLMPKIUGK-UHFFFAOYSA-N
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
PFI-1 efficiently and selectively blocks the interaction of BET BRDs with acetylated histone tails. PFI-1 displaces histone 4 peptide acetylated at lysines K5, K8, K12 and K16 (H4K5acK8acK12acK16ac) with a potency (IC50) of 220nM for BRD4 and 98nM for BRD2. Exposure of sensitive cell lines with PFI-1 results in G1 cell cycle arrest, down-regulation of MYC expression as well as induction of apoptosis and induces differentiation of primary leukaemic blasts.
Product References
  1. Selective inhibition of BET bromodomains: P. Filippakopoulos, et al.; Nature 468, 1067 (2010)
  2. PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains: S. Picaud, et al.; Cancer Res. 73, 3336 (2013)
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