PFI-3 - ≥98%, high purity , CAS No.1819363-80-8, Inhibitor of polybromo 1;Inhibitor of SWI/SNF related; matrix associated; actin dependent regulator of chromatin; subfamily a; member 4
PFI-3 - ≥98%, high purity , CAS No.1819363-80-8, Inhibitor of polybromo 1;Inhibitor of SWI/SNF related; matrix associated; actin dependent regulator of chromatin; subfamily a; member 4
Potent and selective inhibitor of Polybromo (Kd = 48 nM) and SMARCA4 (K d = 89\xa0nM). Also inhibits SMARCA2. Displays high specificity for Family VIII bromodomains. PFI-3 displays selectivity against a range of other kinases.
Storage Temp
Protected from light,Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of polybromo 1;Inhibitor of SWI/SNF related; matrix associated; actin dependent regulator of chromatin; subfamily a; member 4
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Shipped at 4°C. Store at -20°C. Store In the Dark.
1.Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers C et al.. (2016) Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.. J Med Chem, 59 (10):(4800-11). [PMID:27115555][10.1021/op500134e]
2.Fedorov O et al.. (2015) Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.. Sci Adv, 1 (10):(e1500723). [PMID:26702435]
3.Wu Q et al.. (2017) The BRG1 ATPase of human SWI/SNF chromatin remodeling enzymes as a driver of cancer.. Epigenomics, 9 (6):(919-931). [PMID:28521512]
4.Vangamudi B et al.. (2015) The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies.. Cancer Res, 75 (18):(3865-78). [PMID:26139243]
K2214796