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PFI-1

Product ID P2133
Cas No. 1403764-72-6
Purity ≥98%
Product Unit SizeCostQuantityStock
1 mg $52.90 Please Inquire
5 mg $93.80 Please Inquire
10 mg $159.90 Please Inquire
25 mg $303.20 Please Inquire
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  • Product Info
  • Shipping and Storage
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  • References
  • Description
  • Product Info
  • Shipping and Storage
  • Downloads
  • References
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Description

PFI-1 is an inhibitor of BET bromodomains (BRDs) that prevents the association of BET with histones; it acts as an acyl-lysine (Kac) mimetic inhibitor, binding the Kac site of BRD2 and BRD4. PFI-1 exhibits anti-inflammatory and anticancer activities. In H202-treated bronchial epithelial cells, PFI-1 decreases expression of IL-6 and CXCL8. In leukemia cells, PFI-1 downregulates expression of Myc and AurKB, inducing G1 phase cell cycle arrest and suppressing cell growth.

Product Info

Cas No.

1403764-72-6

Purity

≥98%

Formula

C16H17N3O4S

Formula Wt.

347.39

IUPAC Name

2-methoxy-N-(3-methyl-2-oxo-1,4-dihydroquinazolin-6-yl)benzenesulfonamide

Synonym

PF-06405761

Solubility

DMSO 69 mg/mL (198.62 mM) Water Insoluble Ethanol Insoluble

Appearance

White to off white powder

Shipping and Storage

Store Temp

-20°C

Ship Temp

Ambient

Downloads

MSDS

P2133 MSDS PDF

Info Sheet

P2133 Info Sheet PDF

References

Khan YM, Kirkham P, Barnes PJ, et al. Brd4 Is Essential for IL-1β-Induced Inflammation in Human Airway Epithelial Cells. PLoS One. 2014 Apr 23;9(4):e95051. PMID: 24759736.

Picaud S, Da Costa D, Thanasopoulou A, et al. PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains. Cancer Res. 2013 Jun 1;73(11):3336-46. PMID: 23576556.

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