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PFI-1

Item № 11155
CAS № 1403764-72-6
Purity ≥98%
product image
                (CAS 1403764-72-6)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $30.00 0.00
     5 mg $83.00 0.00
     10 mg $135.00 0.00
     25 mg $300.00 0.00

Pricing updated 2019-06-26. Prices are subject to change without notice.

Description
Synonyms
  • PF-06405761

Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of bromodomain-containing protein (BRD) 2 and BRD4 bind acetylated histone tails, which couples histone acetylation marks to the transcriptional regulation of target promoters. Small molecule inhibitors of bromodomain interactions hold promise as useful therapeutics for human disease.1,2,3 PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. In an AlphaScreen assay it has been shown to inhibit BRD2 bromodomain 2 and BRD4 bromodomain 1 with IC50 values of 98 nM and 0.22 μM, respectively. See the Structural Genomics Consortium (SGC) website for more information.

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Technical Information
Formal Name
2-methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide
CAS Number
1403764-72-6
Synonyms
  • PF-06405761
Molecular Formula
C16H17N3O4S
Formula Weight
347.4
Purity
≥98%
Formulation
A crystalline solid
λmax
262 nm
SMILES
O=S(C1=C(OC)C=CC=C1)(NC2=CC=C(NC(N(C)C3)=O)C3=C2)=O
InChI Code
InChI=1S/C16H17N3O4S/c1-19-10-11-9-12(7-8-13(11)17-16(19)20)18-24(21,22)15-6-4-3-5-14(15)23-2/h3-9,18H,10H2,1-2H3,(H,17,20)
InChI Key
TXZPMHLMPKIUGK-UHFFFAOYSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
Downloads & Resources
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Additional Information

View the Cayman Structure Database for chemical structure definitions for many Cayman products

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References & Product Citations
Product Description References

1. Filippakopoulos, P., Qi, J., Picaud, S., et al. Selective inhibition of BET bromodomains Nature 468(7327), 1067-1073 (2010).

2. Hewings, D.S., Wang, M., Philpott, M., et al. 3,5-Dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands Journal of Medicinal Chemistry 54(19), 6761-6770 (2011).

3. Chung, C.W., Coste, H., White, J.H., et al. Discovery and characterization of small molecule inhibitors of the BET family bromodomains Journal of Medicinal Chemistry 54(11), 3827-3838 (2011).

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