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> Pathway Inhibitors>Enzyme Inhibitors>Ubiquitin-Activating Enzyme>FT671

Ubiquitin-Activating Enzyme

FT671 View larger

FT671

AOB37855

CAS No: 1959551-26-8 (S-isomer; Active Isomer)

 

Chemical Name: 5-((1-(4,4-Difluoro-3-(3-fluoro-1H-pyrazol-1-yl)butanoyl)-4-hydroxypiperidin-4-yl)methyl)-1-(4-fluorophenyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one

AOBIOUS launched this product in 2018

CITATIONS - Publications That Use AOBIOUS Product

1) Nat Commun. 2021; 12: 5399.

More details

3990 Items

Alternative choice for FT671 is its analog AOB36638

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HOW TO ORDER

$29.00

$29.00 per mg

Quantity Discount Table - Order More To Get More Price Discount

QuantitymgUnit Price ($/mg or $/Unit)Final Price
15 $24.65 Total: $123.25
110 $20.88 Total: $208.80
125 $17.69 Total: $442.25
150 $15.08 Total: $754.00
1100 $13.05 Total: $1,305.00

Data sheet

Molecular FormulaC24H23F4N7O3
Molecular Weight533.49
CAS Numbers1959551-26-8
Storage Condition0°C (short term), -20°C (long term), desiccated
SolubilityDMSO
Purity98% by HPLC
SynonymFT671; FT 671; FT-671
IUPAC/Chemical Name(S)-5-((1-(4,4-difluoro-3-(3-fluoro-1H-pyrazol-1-yl)butanoyl)-4-hydroxypiperidin-4-yl)methyl)-1-(4-fluorophenyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
InChl KeyBLSNYSFLZAWBIV-SFHVURJKSA-N
InChl CodeInChI=1S/C24H23F4N7O3/c25-15-1-3-16(4-2-15)35-22-17(12-30-35)23(37)33(14-29-22)13-24(38)6-9-32(10-7-24)20(36)11-18(21(27)28)34-8-5-19(26)31-34/h1-5,8,12,14,18,21,38H,6-7,9-11,13H2/t18-/m0/s1
SMILES CodeO=C1C2=C(N=CN1CC3(CCN(CC3)C(C[C@@H](C(F)F)N4N=C(C=C4)F)=O)O)N(N=C2)C5=CC=C(C=C5)F
References1) Turnbull AP, et al. Molecular basis of USP7 inhibition by selective small-molecule inhibitors. Nature. 2017, Oct 26;550(7677):481-486.

2) Preparation of pyrrolo and pyrazolopyrimidines as ubiquitin-​specific protease 7 inhibitors. U.S. Pat. Appl. Publ. (2016), US 20160185785 A1 20160630.

More info

FT671 is a potent, non-covalent, and selective inhibitor of Ubiquitin-Specific Protease 7 (USP7), a deubiquitinating enzyme involved in regulating various cellular processes, including protein stability and signaling pathways.


Mechanism of Action

  • Target: USP7 (also known as HAUSP)

  • Binding Affinity: IC₅₀ of approximately 52 nM; dissociation constant (Kd) of 65 nM

  • Action: FT671 binds to the catalytic domain of USP7, inhibiting its deubiquitinating activity.

Biological Effects

  • Stabilization of p53: By inhibiting USP7, FT671 leads to the destabilization of USP7 substrates, including MDM2, resulting in increased levels of p53 and enhanced transcription of p53 target genes .

  • Cell Cycle Arrest and Apoptosis: FT671 induces G1 phase arrest and apoptosis in various cancer cell lines, such as MM.1S (multiple myeloma) and HCT116 (colorectal cancer) cells .

  • Upregulation of USP22: Inhibition of USP7 by FT671 has been shown to upregulate USP22 protein levels in a dose-dependent manner .ResearchGate+4AACR Journals+4

Preclinical Applications

  • Cancer Research: FT671 has demonstrated efficacy in preclinical models of NRAS-mutant melanoma, delaying tumor growth and enhancing the effects of MEK1/2 inhibitors and anti-PD-1 therapy .

  • Multiple Myeloma: In MM.1S cells, FT671 treatment led to increased p53 levels, MDM2 ubiquitination, and expression of p53 target genes .Synapse+1

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